Dithiolan derivatives, their preparation and their therapeutic effect

ABSTRACT

A compound of formula (I): ##STR1## wherein one of m and n represents 0, and the other represents 0, 1 or 2; k represents 0 or 1 to 12; R 1  is hydrogen, an aryl, a heterocyclic, an alkyl, a hydroxy or --OR 7 , wherein R 7  is an alkyl, an alkenyl or an aralkyl; A is --CON(R 2 )SO 2-- , wherein R 2  is hydrogen, an alkyl or an aralkyl; B is a single bond; and pharmaceutically acceptable salts thereof. The compounds have the ability to enhance the activity of glutathione reductase and can therefore be used for the treatment and prevention of a variety of diseases including cataracts.

BACKGROUND OF THE INVENTION

The present invention relates to a series of new dithiolan derivativeshaving an excellent ability to enhance the activity of glutathionereductase. The invention also provides a process for preparing thesecompounds and methods and compositions using them.

Glutathione is found throughout the tissues of the living body, is amajor reducing agent in cells, and plays a very important role in theoxidation-reduction metabolic processes. In particular, reducedglutathione (GSH), thanks to the presence of a thiol group, plays a keyrole in various cellular defence and repair mechanisms. Glutathioneperoxidase catalyses the reactions involved in these mechanisms, and isan important enzyme in the antioxidant system, wherein perocides (e.g.hydrogen peroxide, lipid peroxides and so on) are reduced by GSH. On theother hand, glutathione reductase is an enzyme which reduces oxidizedglutathione (oxidized-type glutathione; GSSG) in the presence of NADPHto regenerate GSH.

The antioxidant system comprising these materials and enzymes protectscells from the harmful effects of oxidising materials (e.g. abovedescribed peroxides, free radicals and so on). Oxidative stress occurswhen the balance between oxidising materials and the antioxidantmechanisms is shifted in favor of the former [J. Appl. Physiol. 1996November, 81(5), 2199-2202]. It has been reported that oxidative stressis associated with various diseases, such as coronary heart disease,cataracts, pulmonary diseases (e.g., idiopathic pulmonary fibrosis,adult respiratory distress syndrome, emphysema, asthma, bronchopulmonarydysplasia and interstitial pulmonary fibrosis), chronic renal failure,disorders of the nervous system including the peripheral nervous systemand the central nervous system (e.g. Parkinson's disease, schizophrenia,Alzheimer's disease, epilepsy, amyotrophic lateral sclerosis andcerebral ischemia), gastric ulcers, diabetes, hepatocyte necrosis andapoptosis including ethanol-induced hepatopathy, viral disease(including influenza, hepatitis B and HIV), and colorectal cancer [J.Appl. Physiol. 1996 November, 81(5), 2199-2202; Free Radical Biology &Medicine, Vol. 21 No. 6, 845-853 (1996); Free Radical Biology &Medicine, Vol. 20 No. 7, 925-931 (1996); Gastroenterology, 112, 855-863(1997); Free Radical Biology & Medicine, Vol. 34, 161-165 (1996);Lancet, 338, 215-216 (1991); Diabetologia, 39, 357-363 (1996); Eur. J.Cancer., 1996 January, 32A(1), 30-38; Am. J. Med., 1991 September 30.91(3c), 95s-105s; Alcohol. Clin. Exp. Res., 1996 December 20(9 Suppl),340A-346A; Free Radical Biology & Medicine, Vol. 21 No. 5, 641-649(1996); Pharmacol. Toxicol., 1997 April, 80(4), 159-166; Cell. Mol.Biol. (Noisy-le-grand) 1996 February, 42(1), 17-26; Prostaglandins.Leukot. Essent. Fatty Acids, 1996 August, 55(1-2), 33-43; FASEB J., 1995September, 9(12), 1173-1182].

In addition to the above, oxidative stress is thought to be a factor inDown's syndrome, nephritis, pancreatitis, dermatitis, fatigue,rheumatism, various malformations (e.g. Duchenne muscular dystrophy,Becker dystrophy, Dubin-Johnson-Spring syndrome, favism and so on),Fanconi's anemia, canceration and metastases, septicemia, enhancedpermeability of the blood vessels, leukocyte adherence, retinopathy ofprematurity, siderosis, toxic effects of medicines (e.g. carcinostaticsincluding platinum chelate, antibiotics, antiparasitics, paraquat,carbon tetrachloride and halothane) and radiogenic damages [YoshihikoOyanagi, Superoxide dismutase and agents controlling active oxygenspecies].

In WO94/12527, it is disclosed that compounds which enhance thesynthesis of endogenous GSH are suitable for human therapy, inparticular for the treatment of various diseases induced by glutathionedeficiency, such as the pathological states related to oxidative tissuedamage, in particular when resulting from an excess of free radicals.Some examples of such diseases are: intracellular oxidative statedisequilibrium following alcohol abuse, exposure to xenobiotic agents,damage caused by radiation, hepatic diseases, intoxication from drugsand chemical agents, poisoning by heavy metals, physiological brainageing (e.g. Parkinson's disease), brain degeneration due to decreasedglutathione levels caused by altered antioxidant defence mechanisms,such as acute and chronic neurodegenerative diseases (e.g., acutepathologies such as: acute ischemic states, in particular cerebralictus, hypoglycemia, and epileptic attacks; chronic pathologies such as:amyotrophic lateral sclerosis, Alzheimer's disease, Huntington'schorea), diseases related to altered functionality of the immune system,in particular resulting from tumour immunotherapy, and infertility, inparticular male infertility. It is also disclosed that the compounds aresuitable for organ reperfusion following ischemic events mainlyimputable to free radicals.

Furthermore, in Japanese patent publication Kokai Showa 64-26516, it isdisclosed that a compound which increases glutathione levels is usefulfor the treatment and prevention of various diseases includingcataracts, hepatic disorders, nephritic disorders.

At this time, lipoic acid (thioctic acid), which has dithiolan ring inits molecule, is known to influence the biosynthesis and regeneration ofreduced glutathione [I. Maitra et al., Free Radical Biology & Medicine,Vol. 18 No. 4, 823-829 (1995)]. In this literature, it is reported thatthe total glutathhione (oxidized and reduced glutathione) level isdecreased by administering buthionine sulfoximine (BSO), which is aninhibitor of glutathione synthetase, to newborn rats, that the decreaseis prevented by administering lipoic acid together with BSO, and thatcataract formation is suppressed. In addition, the literature describesa test on the effects on glutathione reductase achieved by administeringonly BSO or by administering both BSO and lipoic acid. Considering theseresults, it is understood that the activity of glutathione reductasedoes not change when BSO is simply administered by itself, and that theactivity of glutathione reductase also does not increase when lipoicacid is administered in addition to BSO.

It can, therefore, be deduced from this literature that the totalglutathione level will be increased and that disorders can be treatedwhen lipoic acid is administered to a patient who is suffering from adisease caused by a deficiency of glutathione synthesis, but lipoic acidis not thought to provide sufficient effect against diseases which occurin spite of enough glutathione synthesis since it is understood not toincrease glutathione reductase activity.

On the contrary, if the activity of glutathione reductase can beincreased, then whether glutathione synthesis is or is not adequate,diseases which occur in spite of enough glutathione synthesis and whichare caused by oxidative stress can be prevented or treated since thesupply of reduced glutathione is increased.

Furthermore, in general, in the case of ophthalmologic diseases, such ascataracts, topical application to the eyes is preferred to oraladministration. However, since lipoic acid is a powerful stimulant, itis impossible to administer it to the eyes.

We have now discovered a series of dithiolan derivatives, which have theability to cause a significant increase in the activity of glutathionereductase and which also remove peroxides. Moreover, the compounds ofthe present invention are less stimulating to the eyes than lipoic acidand similar known compounds are thus especially suitable for topicalapplication.

For the avoidance of doubt, the compounds of the present invention arenamed following the IUPAC Rules, using, as appropriate, lipoic acid(also known as thioctic acid) as the parent compound. This compound hasthe formula: ##STR2##

It is an object of the present invention to provide a series of newdithiolan derivatives.

It is a further and more specific object of the present invention toprovide such compounds which increase the activity of glutathionereductase.

BRIEF SUMMARY OF INVENTION

The compounds of the present invention are those compounds of formula(I): ##STR3## wherein:

one of m and n represents 0, and the other represents 0, 1 and 2;

k represents 0 or an integer of from 1 to 12;

R¹ represents:

a hydrogen atom,

a group selected from substituents α, defined below, or

an alkyl group having from 1 to 12 carbon atoms which is unsubstitutedor is substituted by from 1 to 3 substituents selected from the groupconsisting of substitutents α and the substituents γ or such asubstituted or unsubstituted alkyl group in which the carbon chain isinterrupted by an oxygen atom and/or a sulfur atom;

A represents a single bond, an oxygen atom, a carbonyl group or a groupof formula --N(R²)CO--, --N(R²)CS--, --N(R²)SO₂ --, --CON(R²)N(R³)CO--,--CON(R²)CO--, --CON(R²)CS--, --CON(R²)SO₂ --, --O--CO--, --ON(R²)CO--,--ON(R²)SO₂ --, --O--CON(R²)N)R³ CO--, --O--CON(R²)CO--, --O--CON(R²)SO₂--, --CO--O--, --CO--CO--, --CO--CON(R²)N(R³)CO--, --CO--CON(R²)CO--,--CO--CON(R²)SO₂ --, --N(R²)O--, --N(R²)COCO--, --N(R²)N(R³)CO--,--N(R²)N(R³)SO₂ --, --N(R²)CON(R³)N(R⁴)CO--, --N(R²)CON(R³)CO--,--N(R²)CON(R³)SO₂ --, or --N(R²)CON(R³)SO₂ N(R⁴)CO--

wherein R², R³ and R⁴ are the same or different and each represents ahydrogen atom, an alkyl group having from 1 to 12 carbon atoms, anaralkyl group, an aralkyl group of which the aryl moiety is substitutedwith from 1 to 3 groups selected from the group consisting ofsubstituents β, an acyl group or a group selected from the groupconsisting of substituents α;

B represents a single bond, or a group of formula --N(R⁵)-- or--N(R⁶)N(R⁵)--

wherein R⁵ and R⁶ are the same or different and each represents ahydrogen atom, an alkyl group having from 1 to 12 carbon atoms, anaralkyl group, an aralkyl group of which the aryl moiety is substitutedwith from 1 to 3 groups selected from the group consisting ofsubstituents β, an acyl group or a group selected from the groupconsisting of substituents α, or R⁵, together with R¹ and the nitrogenatom to which they are bonded, may form a heterocyclic ring having from5 to 7 ring atoms;

or, where A represents a group of formula --N(R²)CO--, --N(R²)CS--,--CON(R²)N(R³)CO--, --CON(R²)CO--, --CON(R²)CS--, --O--CO--,--ON(R²)CO--, --O--CON(R²)N(R³)CO--, --O--CON(R²)CO--,--CO--CON(R²)N(R³)CO--, --CO--CON(R²)CO--, --N(R²)N(R³)CO--,--N(R²)CON(R³)N(R⁴)CO-- or --N(R²)CON(R³)CO-- [wherein R², R³ and R⁴ areas defined above] and B represents a single bond, R¹ may represent agroup of formula --OR⁷ (wherein R⁷ represents a lower alkyl group, alower alkenyl group, an aralkyl group, an aralkyl group of which thearyl moiety is substituted with 1 to 3 groups selected from the groupconsisting of substituents β or a group selected from the consisting ofsubstituents α);

or, where A represents a group of formula --CON(R²)SO₂ --, --ON(R²)SO₂--, --O--CON(R²)SO₂ --, --CO--CO--, --CO--CON(R²)SO₂ --, --N(R²)COCO--,--N(R²)N(R³)SO₂ --, or --N(R²)CON(R³)SO₂ -- [wherein R² and R³ are asdefined above ] and B represents a single bond, or, where A does notrepresent an oxygen atom, a group of formula --CO--O-- or --N(R⁶)O-- andB represents --N(R⁵)-- [wherein R⁵ is as defined above], R¹ mayrepresent a hydroxy group or a group of formula --OR⁷ (wherein R⁷ is asdefined above);

Substituents α are selected from the group consisting of aryl groups,heterocyclic groups, aryl groups substituted with from 1 to 3 ofsubstituents β, and heterocyclic groups substituted with from 1 to 3 ofsubstituents β;

Substituents β are selected from the group consisting of lower alkylgroups, halogenated lower alkyl groups, lower alkoxy groups, loweralkylthio groups, hydroxy groups, carboxy groups, carbamoyl groups ofwhich the nitrogen atom may be substituted, lower alkoxycarbonyl groups,halogen atoms, nitro groups, amine residues, sulfo groups, sulfamoylgroups, cyano groups, hydroxy-substituted lower alkyl groups;

Substituents γ are selected from the group consisting of lower alkoxygroups, lower alkylthio groups, hydroxy groups, nitrooxy groups, carboxygroups, lower alkoxycarbonyl groups, halogen atoms, sulfo groups,sulfamoyl groups, amine residues, carbamoyl groups of which the nitrogenatom may be substituted;

PROVIDED THAT:

where A represents an oxygen atom, B represents a single bond or a groupof formula --N(R⁵)-- [wherein R⁵ is as defined above],

where A represents a group of formula --CO--O-- or --N(R²)O-- [whereinR² is as defined above], B represents a single bond, and

where k represents 4, the group of formula --A--B--R¹ does not representa carboxyl group

and pharmaceutically acceptable salts thereof.

The present invention also provides a method of enhancing the activityof glutathione reductase in a mammal, which may be human, byadministering to said mammal an effective amount of a compounds offormula (I) or a pharmaceutically acceptable salt thereof.

The present invention also provides a method for the treatment orprevention of cataract in a mammal, which may be human, by administeringto said mammal an effective amount of a compounds of formula (I) or apharmaceutically acceptable salt thereof.

DETAILED DESCRIPTION OF INVENTION

In the compounds of the present invention, one of m and n represents 0,and the other represents 0, 1 or 2. Preferably, either both of m and nrepresent 0, or one of m and n represents 0 and the other represents 1.More preferably, both of m and n represent 0.

We prefer those compounds of formula (I) wherein k represents 0 or aninteger of from 1 to 6, more preferably an integer of from 2 to 6, andmost preferably an integer of from 4 to 6.

Where R¹ or substituent α represents an aryl group, this is acarbocyclic aromatic hydrocarbon group having from 6 to 14 ring carbonatoms in one or more aromatic carbocyclic rings or is such a group whichis fused to a cycloalkyl group having from 3 to 10 ring carbon atoms,Examples of carbocyclic aromatic hydrocarbon groups having from 6 to 14ring carbon atoms in one or more aromatic carbocyclic rings include thephenyl, naphthyl (1- or 2-naphthyl), phenanthrenyl and anthracenylgroups. An example of a group in which an aromatic carbocyclic ring isfused to a cycloalkyl group is the 2-indanyl group.

Where R¹ or substituent α represents a heterocyclic group, this has from5 to 7 ring atoms of which from 1 to 3 are hetero-atoms selected fromthe group consisting of sulfur, oxygen and nitrogen hetero-atoms. Thegroup may be saturated or it may be unsaturated and preferably aromatic.

Where the heterocyclic groups referred to herein have 3 hetero-atoms, weprefer that all three, two or one of these atoms are nitrogen atoms,and, correspondingly, none, one or two are sulfur and/or oxygen atoms.

Examples of such saturated heterocyclic groups include, for example, thepyrrolidinyl, imidazolidinyl, pyrazolidinyl, oxazolidinyl,isoxazolidinyl, thiazolidinyl, isothiazolidinyl, dithiolanyl,thiadiazolidinyl, oxadiazolidinyl, dithiazolidinyl, piperidyl,piperazinyl, morpholinyl, thiomorpholinyl dioxanyl and homopiperazinylgroups. Of these groups, we particularly prefer those 5- to 7-memberedsaturated heterocyclic groups which have one or two nitrogen atoms orhave one nitrogen atom and one sulfur atom or one oxygen atom, such asthe pyrrolidinyl, thiazolidinyl, imidazolidinyl, piperidyl, morpholinyl,thiomorpholinyl and piperazinyl groups.

If desired, the above-described saturated heterocyclic groups may besubstituted by one or two atoms selected from the group consisting ofsulfur atoms and oxygen atoms to form an oxo group and/or a thioxogroup. Examples of such groups include the piperidonyl, pyrrolidonyl,thiazolidonyl, dioxothiazolidinyl, thioxodithiazolidinyl,dioxomidazolidinyl and dioxooxazolidinyl groups.

Also, if desired, the above-described saturated heterocyclic group maybe fused with another cyclic group, preferably having 3, 4, 5 or 6 ringatoms, and which may be carboxyxlic or heterocyclic, most preferably abenzene ring. Examples of such fused ring groups include thebenzodioxanyl, indolinyl, isoindolinyl, benzooxazinyl,benzothiazolidinyl, benzothiazinyl, chromanyl,6-acetoxy-2,5,7,8-tetramethylchroman-2-yl, and isoindol-1,3-dion-2-ylgroups.

Examples of such aromatic heterocyclic groups include the furyl,thienyl, pyrrolyl, azepinyl, pyazolyl, imidazolyl, oxazolyl, isoxazolyl,thiazolyl, isothiazolyl, oxadiazolyl, triazolyl, tetrazolyl,thiadiazolyl, pyranyl, pyridyl, pyridazinyl, pyrimidinyl and pyrazinylgroups. Of these, those 5- to 7-membered aromatic heterocyclic groupswhich have at least one nitrogen atom and may have an oxygen atom or asulfur atom are preferred. Examples of such groups include the pyrrolyl,azepinyl, pyrazolyl, imidazolyl, oxazolyl, isoxazolyl, thiazolyl,isothiazolyl, oxadiazolyl, triazolyl, tetrazolyl, thiadiazolyl, pyridyl,pyridazinyl, pyrimidinyl and pyrazinyl groups. The pyridyl, imidazolyl,oxazolyl, pyrazinyl and thiazolyl groups are most preferred.

Also, if desired, the above-described aromatic heterocyclic group may befused with another cyclic group, preferably having 3, 4, 5 or 6 ringatoms, and which may be carbocyclic or heterocyclic, most preferably abenzene ring. Examples of such fused ring groups include the indolyl,benzofuryl, benzothienyl, benzooxazolyl, benzoimidazolyl, quinolyl,isoquinolyl, quinoxalyl groups.

Also, the above-described aromatic heterocyclic groups may besubstituted by one or two atoms selected from the group consisting ofsulfur atoms and oxygen atoms to form an oxo group and/or a thioxogroup, and examples of such groups include the pyridonyl, oxazilonyl,pyrazolonyl, isoxazolonyl and thioxodithiazolyl groups.

If desired, any of the above aryl and heterocyclic groups may besubstituted by one of more, preferably from 1 to 3, substituent selectedfrom the group consisting of substituents β, defined above andexemplified below.

Where R¹ represents an alkyl group having from 1 to 12 carbon atoms,this may be a straight or branched chain group which may beunsubstituted or may be substituted by from 1 to 3 substituents selectedfrom the group consisting of substituents γ, defined above andexemplified below. Examples of such unsubstituted alkyl groups includethe methyl, ethyl, propyl, isopropyl, butyl, isobutyl, sec-butly,t-butyl, pentyl, 2-pentyl, 3-pentyl, 2-methylbutyl, 3-methylbutyl,1,1-dimethylpropyl, 1,2-dimethylpropyl, 2,2-dimethylpropyl, hexyl,2-hexyl, 3-hexyl, 2-methylpentyl, 3-methylpentyl, 4-methylpentyl,1,1-dimethylbutyl, 1,2-dimethylbutyl, 1,3-dimethylbutyl,2,2-dimethylbutyl, 2,3-dimethylbutyl, 3,3-dimethylbutyl,1,1,2-trimethylpropyl, 1,2,2-trimethylpropyl, heptyl, 2-heptyl,3-heptyl, 4-heptyl, 3,3-dimethylpentyl, octyl, 2-methylhepty,2-ethylhexyl, 1,1,3,3-tetramethylbutyl, nonyl, 2-nonyl, 3-nonyl,4-nonyl, 5-nonyl, 2-methyloctyl, 3-methyloctyl, 4-methyloctyl,5-methyloctyl, 6-methyloctyl, 7-methyloctyl, 8-methyloctyl,6,6-dimethylheptyl, decyl, 2-decyl, 3-decyl, 4-decyl, 5-decyl,2-methylnonyl, 3-methylnonyl, 4-methylnonyl, 6,6-dimethyloctyl, undecyl,2-undecyl, 3-undecyl, 4-undecyl, 5-undecyl, 6-undecyl, 2-methyldecyl,3-methyldecyl, 4-methyldecyl, 5-methyldecyl, 6-methyldecyl,7-methyldecyl, 8-methyldecyl, 9-methyldecyl, 7-ethynonyl, dodecyl,2-dodecyl, 3-dodecyl, 4-dodecyl, 5-dodecyl, 6-dodecyl, 2-methylundecyl,3-methylundecyl, 4-methylundecyl, 5-methylundecyl, 6-methylundecyl,7-methylundecyl, 8-methylundecyl, 9-methylundecyl and 10-methylundecylgroups. Of these, straight or branched alkyl groups having from 1 to 6carbon atoms are preferred, straight or branched alkyl groups havingfrom 1 to 4 carbon atoms are more preferred, and the methyl, ethyl,propyl, isopropyl, butyl, isobutyl, and t-butyl groups are mostpreferred.

Alternatively, R¹ may represent such an alkyl group in which the carbonchain is interrupted by one or more oxygen atoms and/or sulfur atoms.Examples of such groups include any of the above alkyl groups which aresubstituted by a single alkoxy or alkylthio group, which itself may befurther substituted by an alkoxy or alkylthio group, the alkoxy andalkylthio groups being as exemplified below in relation to substituentsβ and γ. Specific examples of such groups include alkoxyalkyl groupshaving from 2 to 10 carbon atoms, alkylthioalkyl groups having from 2 to10 carbon atoms, benzyloxyalkyl groups of which the alkyl part has from1 to 5 carbon atoms and benzylthioalkyl groups of which the alkyl parthas from 1 to 5 carbon atoms (the benzyl part of the benzyloxyalkyl andbenzylthoalkyl groups may be unsubstituted or substituted with from 1 to3 substituents selected from the group consisting of substituents β)groups. Of these, the methoxymethyl, methoxyethyl, ethoxymethyl,methylthiomethyl, methylthioethyl, ethylthiomethyl, benzyloxymethyl,benzyloxyethyl, benzylthiomethyl and 4-methoxybenxylthiomethyl groupsare preferred.

Where R², R³, R⁴, R⁵ and R⁶ represents an alkyl group having from 1 to12 carbon atoms, this may be straight or branched chain group, asdefined and exemplified above in relation to R¹,

Where R², R³, R⁴, R⁵ and R⁶ represents an aralkyl group, this is a loweralkyl group (preferably having from 1 to 6 carbon atoms, more preferablyfrom 1 to 4 carbon atoms, still more preferably from 1 to 3 carbon atomsand most preferably 1 or 2 carbon atoms) which is substituted by from 1to 3 aryl groups as defined and exemplified above in relation to R¹.Specific examples of such aralkyl groups include the benzyl,1-phenylethyl, 2-phenylethyl, α-naphthylmethyl, β-naphthylmethyl,diphenylmethyl, triphenylmethyl, α-naphthyldiphenylmethyl and9-anthrylmethyl groups. Of these, the benzyl, 1-phenylethyl and2-phenylethyl groups are preferred. Any of the above groups may beunsubstituted or it may be substituted by from 1 to 3 substituentsselected from the group consisting of substituents γ defined andexemplified below.

Where R², R³, R⁴, R⁵ and R⁶ represents an acyl group, this may be analiphatic, aromatic or heterocyclic acyl group, for example:

an alkylcarbonyl group having from 1 to 30, preferably from 1 to 21 andmore preferably from 1 to 8 carbon atoms, such as the formyl, acetyl,propionyl, butyryl, isobutyryl, pivaloyl, valeryl, isovaleryl, octanoyl,nonylcarbonyl, decylcarbonyl, 3-methylnonylcarbonyl,8-methylnonylcarbonyl, 3-ethyloctylcarbonyl, 3,7-dimethyloctylcarbonyl,undecylcarbonyl, dodecylcarbonyl, tridecylcarbonyl, tetradecylcarbonyl,pentadecylcarbonyl, hexadecylcarbonyl, 1-methylpentadecylcarbonyl,14-methylpentadecylcarbonyl, 13,13-dimethyltetradecylcarbonyl,heptadecylcarbonyl, 15-methylhexadecylcarbonyl, octadecylcarbonyl,1-methylheptadecylcarbonyl, nonadecylcarbonyl, eicosylcarbonyl andheneicosylcarbonyl groups; of these, the groups having from 1 to 5carbon atoms are most preferred;

a halogenated alkylcarbonyl group having from 2 to 6 carbon atoms,preferably 2 or 3 carbon atoms, such as the chloroacetyl,dichloroacetyl, trichloroacetyl and trifluoroacetyl groups;

a lower alkoxyalkylcarbonyl group in which the alkyl and alkoxy partseach preferably has from 1 to 4 carbon atoms, such as the methoxyacetylgroup;

an unsaturated alkylcarbonyl group having from 3 to 6 carbon atoms, suchas the acryloyl, propioloyl, methacryloyl, crotonoyl, allylcarbonyl,isocrotonoyl and (E)-2-methyl-2-butenoyl groups;

an arylcarbonyl group, such as the benzoyl, α-naphthoyl and β-naphthoylgroups;

a halogenated arylcarbonyl group, such as the 2-bromobenzoyl and4-chlorobenzoyl groups;

a lower alkyl-substituted arylcarbonyl group, such as the2,4,6-trimethylbenzoyl and 4-toluoyl groups;

a hydroxy-substituted arylcarbonyl group, such as the3,5-dimethyl-4-hydroxybenzoyl and 3,5-di-t-butyl-4-hydroxybenzoylgroups;

a lower alkoxy-substituted arylcarbonyl group, such as the 4-anisoylgroup;

a nitro-substituted arylcarbonyl group such as the 4-nitrobenzoyl and2nitrobenzoyl groups;

a lower alkoxycarbonyl-substituted arylcarbonyl group, such as the2-(methoxycarbonyl)benzoyl group;

an aryl-substituted arylcarbonyl group, such as the 4-phenylbenzoylgroup;

a lower alkoxycarbonyl group preferably having from 2 to 7 carbon atoms,such as the methoxycarbonyl, ethoxycarbonyl, propoxycarbonyl,butoxycarbonyl, sec-butoxycarbonyl, t-butoxycarbonyl andisobutoxycarbonyl groups;

a lower alkoxycarbonyl group, preferably having from 2 to 7 carbonatoms, which is substituted with a halogen atom or a tri-loweralkylsilyl group, such as the 2,2,2-trichloroethoxycarbonyl and 2-trimethylsilylethoxycarbonyl groups;

an aralkylcarbonyl group, of which the aryl ring may be unsubstituted ormay be substituted with 1 or 2 lower alkoxy or nitro groups, such as thebenzylcarbonyl, 4-methoxybenzylcarbonyl, 3,4-dimethoxybenzylcarbonyl,2-nitrobenzylcarbonyl and 4-nitrobenzylcarbonyl groups;

a lower alkanesulfonyl group, preferably having from 1 to 6 carbonatoms, such as the methanesulfonyl, ethanesulfonyl and propanesulfonylgroups;

a halogenated lower alkanesulfonyl group, preferably having from 1 to 6carbon atoms, such as the chloromethanesulfonyl,trifluoromethanesulfonyl and pentafluoroethanesulfonyl groups; and

an arylsulfonyl group, in which the aryl part is as defined andexemplified above in relation to R¹, such as the benzenesulfonyl andp-toluenesulfonyl group.

Of the above groups, we prefer the aliphatic acyl groups, the aromaticacyl groups, the alkoxycarbonyl groups and the lower alkanesulfonylgroups, more preferably the alkylcarbonyl groups and the loweralkoxycarbonyl groups.

Where R⁵, together with R¹ and the nitrogen atom to which they areattached forms a heterocyclic group, this has from 5 to7, morepreferably 5 or 6, ring atoms of which from 1 to 3 are hetero-atomsselected from the group consisting of nitrogen, oxygen and sulfur atoms,at least one being a nitrogen atom. Preferably there are one or twonitrogen atoms and no or one oxygen atoms or sulfur atoms. Examples ofsuch groups include the pyrrolidino, 3-thiazolidinyl, piperidino,piperazino, morpholino, thiomorpholino, homopiperazino, imidazolidinyland imidazolyl groups. Such groups may be substituted or unsubstituted,preferably with one or two oxygen atoms and/or with 1 to 3 substituentsselected from the group consisting of substituents β, as defined above,and may be fused with another cyclic group, preferably having 3, 4, 5 or6 ring atoms, and which may be carbocyclic or heterocyclic, mostpreferably a benzene ring. Examples of such groups are theN-methylpiperazino, N-t-butoxycarbonylpiperazino, 1-indolinyl,2-carboxy-1-indolinyl, 2-methoxycarbonyl-1-indolinyl,3,4-dimethylindolin-2,5-dione-1-yl and isoindol-1,3-dion-2-yl groups.

Where R⁷ or substituent β represents lower alkyl group, this may be astraight or branched chain group having from 1 to 6, preferably from 1to 4, carbon atoms, and examples include the methyl, ethyl, propyl,isopropyl, butyl, isobutyl, sec-butyl, t-butyl, pentyl, isopentyl,neopentyl, 2-methylbutyl, 1-ethylpropyl, hexyl, isohexyl,4-methylpentyl, 3-methylpentyl, 2-methylpentyl, 1-methylpentyl,3,3-dimethylbutyl, 2,2-dimethylbutyl, 1,1-dimethylbutyl,1,2-dimethylbutyl, 1,3-dimethylbutyl, 2,3-dimethylbutyl and 2-ethylbutylgroups. Of these, we prefer those alkyl groups having from 1 to 4 carbonatoms, particularly the methyl, ethyl, propyl, isopropyl, butyl,isobutyl and t-butyl groups, and most preferably the methyl group.

Where R⁷ represents a lower alkenyl group, this may be a straight orbranched chain group having from 2 to 6, preferably 3 or 4, carbonatoms, and examples include the vinyl, allyl, methallyl, 1-propenyl,isoprepenyl, 1-butenyl, 2-butenyl, 3-butenyl, 1-pentenyl, 2-pentenyl,3-pentenyl, 4-pentenyl, 1-hexenyl, 2-hexenyl, 3-hexenyl and 4-hexenylgroups, of which the vinyl, allyl, methallyl, 1-propenyl, isopropenyland butenyl groups are preferred, the allyl and 2-butenyl groups beingmost preferred.

Where R⁷ represents an aralkyl group, this may be any of the aralkylgroups defined and exemplified above in relation to R².

Where substituent β represents a halogenated lower alkyl group, this maybe any of the above alkyl groups which is substituted by at least onehalogen atom. Although there is no critical limitation on the number ofhalogen substituents, and the group may, if desired, be perhalogenated,in general, from 1 to 3 halogen atoms, selected from the groupconsisting of fluorine, chlorine, bromine and iodine atoms arepreferred. Examples of such haloalkyl groups include the chloromethyl,dichloromethyl, trichloromethyl, trifluoromethyl, 2-chloroethyl,2-fluoroethyl, 2-bromoethyl, 2-iodoethyl, 2,2,2-trichloroethyl,2,2,2-trifluoroethyl, 3-chloropropyl, 3-fluoropropyl, 3-bromopropyl,3-iodopropyl, 3,3,3-trichloropropyl, 3,3,3-trifluoropropyl,4-chlorobutyl, 4-fluorobutyl, 4-bromobutyl and 4-iodobutyl groups.

Where substituent β or substituent γ represents a lower alkoxy group,this may be a straight or branched chain group having from 1 to 6,preferably from 1 to 4, carbon atoms, and examples include the methoxy,ethoxy, propoxy, isopropoxy, butoxy, isobutoxy, sec-butoxy, t-butoxy,pentyloxy, isopentyloxy, neopentyloxy, 2-methylbutoxy, 1-ethylpropoxy,hexyloxy, isohexyloxy, 3-methylpentyloxy, 2-methylpentyloxy,1-methylpentyloxy, 3,3-dimethylbutoxy, 2,2-dimethylbutoxy,1,1-dimethylbutoxy, 1,2-dimethylbutoxy, 1,3-dimethylbutoxy,2,3-dimethylbutoxy and 2-ethylbutoxy groups. Of these, we prefer thosealkoxy groups having from 1 to 4 carbon atoms, particularly the methoxy,ethoxy, propoxy, isopropoxy, butoxy and t-butoxy groups, and mostpreferably the methoxy group.

Where substituent β or substituent γ represents a lower alkylthio group,this may be a straight or branched chain group having from 1 to 6,preferably from 1 to 4, carbon atoms, and examples include themethylthio, ethylthio, propylthio isopropylthio, butylthio,isobutylthio, sec-butylthio, t-butylthio, pentylthio, isopentylthio,neopentylthio, 2-methylbutylthio, 1-ethylpropylthio, hexylthio,isohexylthio, 4-methylpentylthio, 3-methylpentylthio,2-methylpentylthio, 1-methylpentylthio, 3,3-dimethylbutylthio,2,2-dimethylbutylthio, 1,1-dimethylbutylthio, 1,2-dimethylbutylthio,1,3-dimethylbutylthio, 2,3-dimethylbutylthio and 2-ethylbutylthiogroups. Of these, we prefer those alkylthio groups having from 1 to 4carbon atoms, particularly the methylthio, ehtyltho, propylthio,isopropylthio, butylthio and isobutylthio groups, and most preferablythe methylthio group.

Where substituent β or substituent γ represents an amine residue, thisis a group of formula --NR^(a) R^(b), where R^(a) and R^(b) are the sameor different and each represents a hydrogen atom, a lower alkyl group(as defined and exemplified above in relation to R⁷ or substituent β), acycloalkyl group having from 3 to 8, preferably 5 or 6, ring carbonatoms, an aryl group (as defined and exemplified above in relation toR¹), an aralkyl group (as defined and exemplified above in relation toR²), a heterocyclic group (as defined and exemplified above in relationto R¹), or R^(a) and R^(b) together with the nitrogen atom to which theyare attached represent a nitrogen-containing heterocyclic group (asdefined and exemplified above in relation to R⁵ and R¹). Examples ofsuch groups include:

the amino group;

alkylamino and dialkylamino groups, such as the methylamino, ethylamino,isopropylamino, butylamino, dimethylamino, diethylamino,diisopropylamino and ditubylamino groups;

cycloalkylamino and dicycloalkylamino groups, such as thecyclopentylamino, cyclohexylamino, dicyclopentylamino anddicyclohexylamino groups;

saturated cyclic amino groups, that is heterocyclic groups having anitrogen atom in the ring, such as the pyrrolidino, piperidino,piperazino, N-methylpiperazino, morpholino and thiomorpholino groups;

aryl- and aralkylamino groups of which the nitrogen atom may besubstituted with a lower alkyl group, such as the anilino, benzylamino,N-methylanilino and N-methylbenzylamino groups; and

a heterocyclic-substituted amino group, in which the nitrogen atom maybe substituted with a lower alkyl group, such as the pyridylamino,N-methylpyridylamino and N-ethylpyridylamino groups.

Of these, we prefer the amino group, mono- and di-alkylamino groups,saturated cyclic amino groups (such as the pyrrolidino, piperidino,piperazino, N-methylpiperazino, morpholino and thiomorpholino groups)and aryl- and aralkylamino groups of which the nitrogen atom may besubstituted with a lower alkyl group (such as the anilino, benzylamino,N-methylanilino and N-methylbenzylamino groups).

Where substituent β or substituent γ represents a carbamoyl group ofwhich the nitrogen atom may be substituted, this is a group of formula--CONR^(a') R^(b'), where R^(a') and R^(b') are the same or differentand each represents any of the atoms or groups represented by R^(a) andR^(b) or a one of R^(a) and R^(b) represents a hydrogen atom and theother represents an acyl group (which may be any of the acyl groupsdefined and exemplified above in relation to R²) or an aminosulfonylgroup. Examples of such carbamoyl groups include:

the carbamoyl group;

alkylcarbamoyl and dialkylcarbamoyl groups, such as the methylcarbamoyl,ethylcarbamoyl, isopropylcarbamoyl, butylcarbamoyl, dimethylcarbamoyl,diethylcarbamoyl, diisopropylcarbamoyl and dibutylcarbamoyl groups;

cycloalkylcarbamoyl and dicycloalkylcarbamoyl groups, such as thecyclopentylcarbamoyl, cyclohexylcarbamoyl, dicyclopentylcarbamoyl anddicyclohexylcarbamoyl groups;

saturated cyclic aminocarbonyl groups, that is carbonyl groups attachedto a heterocyclic group having a nitrogen atom in the ring, such as thepyrrolidinocarbonyl, piperidinocarbonyl, piperazinocarbonyl,N-methylpiperazinocarbonyl, morpholinocarbonyl andthiomorpholinocarbonyl groups;

aryl- and aralkylcarbamoyl groups of which the nitrogen atom may besubstituted with a lower alkyl group, such as the phenylcarbamoyl,benzylcarbamoyl, N-methylphenylcarbamoyl and N-methylbenzylcarbamoylgroups;

a heterocyclic-substituted carbamoyl group, in which the nitrogen atommay be substituted with a lower alkyl group, such as thepyridylcarbamoyl, N-methylpyridylcarbamoyl and N-ethylpyridylcarbamoylgroups; and

acylcarbamoyl groups, especially alkanesulfonylaminocarbonyl groups,such as the methanesulfonylaminocarbonyl group and theaminosulfonylaminocarbonyl group.

Of these, we prefer the carbamoyl group, mono- and di-alkylcarbamoylgroups, saturated cyclic carbamoyl groups (such as thepyrrolidinocarbonyl, piperidinocarbonyl, piperazinocarbonyl,N-methylpiperazinocarbonyl, morpholinocarbonyl andthiomorpholinocarbonyl groups), aryl- and aralkylcarbamoyl groups ofwhich the nitrogen atom may be substituted with a lower alkyl group(such as the phenylcarbamoyl, benzylcarbamoyl, N-methylphenylcarbamoyland N-methylbenzylcarbamoyl groups) or an alkanesulfonylaminocarbonylgroup (such as the methanesulfonylaminocarbonyl group).

Where substituent β or substituent γ represents a lower alkoxycarbonylgroup, this may be a straight or branched chain group having from 1 to6, preferably from 1 to 4, carbon atoms in the alkoxy part (i.e. from 2to 7 carbon atoms in the alkoxycarbonyl part), and examples include themethoxycarbonyl, ethoxycarbonyl, propoxycarbonyl, isopropoxycarbonyl,butoxycarbonyl, isobutoxycarbonyl, sec-butoxycarbonyl, t-butoxycarbonyl,pentyloxycarbonyl, isopentyloxycarbonyl, neopentyloxycarbonyl,2-methylbutoxycarbonyl, 1-ethylpropoxycarbonyl, hexyloxycarbonyl,isohexyloxycarbonyl, 4-methylpentyloxycarbonyl,3-methylpentyloxycarbonyl, 2-methylpentyloxycarbonyl,1-methylpentyloxycarbonyl, 3,3-dimethylbutoxycarbonyl,2,2-dimethylbutoxycarbonyl, 1,1-dimethylbutoxycarbonyl,1,2-dimethylbutoxycarbonyl, 1,3-dimethylbutoxycarbonyl,2,3-dimethylbutoxycarbonyl and 2-ethylbutoxycarbonyl groups. Of these,we prefer those alkoxycarbonyl groups having from 1 to 4 carbon atoms,particularly the methoxycarbonyl, ethoxycarbonyl, propoxycarbonyl,isopropoxycarbonyl, butoxycarbonyl and t-butoxycarbonyl groups, and mostpreferably the methoxycarbonyl group.

Where substitutent β or substitutent γ represents a halogen atom, thismay be a fluorine, chlorine, bromine or iodine atom, preferably afluorine or chlorine atom.

Where substituent β represents a hydroxy-substituted lower alkyl group,this may be any of the lower alkyl groups defined and exemplified abovein relation to R² which is substituted by one or more hydroxy groups.Examples of such groups include the hydroxymethyl, hydroxyethyl,hydroxypropyl and hydroxybutyl groups.

Of the compounds of the present invention, those compounds of formula(I) in which the group of formula --(CH₂)_(k) --ABR¹ is bonded to the3-positin of the dithiolan ring are preferred. Such compounds may berepresented by the formula (I'): ##STR4## in which A, B, R¹, k, m and nare as defined above).

Where the compounds of the present invention possess a basic group, suchas an amino or imino group, the compounds can form salts with acids. Onthe other hand, where the compounds of the present invention possess anacidic group, such as a carboxy group or an imido group, they can formsalts with bases. There is no particular restriction on the nature ofsuch salts, provided that, where they are intended for pharmaceuticaluse, they are pharmaceutically acceptable, that is they are not lessactive (or unacceptably less active) than the compound of formula (I),and are not more toxic (or unacceptably more toxic) than the compound offormula (I).

Examples of such salts formed between a basic group in the compound ofthe present invention and an acid include: salts with mineral acids,especially hydrohalic acids (such as hydrofluoric acid, hydrobromicacid, hydroiodic acid or hydrochloric acid), nitric acid, perchloricacid, carbonic acid, sulfuric acid or phosphoric acid; salts with loweralkylsulfonic acids, such as methanesulfonic acid,trifluoromethanesulfonic acid or ethanesulfonic acid; salts witharylsulfonic acids, such as benzenesulfonic acid or p-toluenesulfonicacid; salts with organic carboxylic acids, such as acetic acid, fumaricacid, tartaric acid, oxalic acid, maleic acid, malic acid, succinicacid, benzoic acid, mandelic acid, ascorbic acid, lactic acid, gluconicacid or citric acid; and salts with amino acids, such as glycine,lysine, arginine, ornithine, glutamic acid or aspartic acid.

Examples of such salts formed between an acidic group in the compound ofthe present invention and a base include: salts with an alkali metal,such as sodium, potassium or lithium; salts with an alkaline earthmetal, such as barium or calcium; salts with another metal, such asmagnesium, aluminum or ion; ammonium salts; organic base salts, such asa salt with t-octylamine, dibenzylamine, morpholine, glucosamine, aphenylglycine alkyl ester, ethylenediamine, N-methylglucamine,guanidine, methylamine, dimethylamine, diethylamine, triethylamine,diisopropylamine, cyclohexylamine, dicyclohexylamine,N,N-dibenzylethylenediamine, chloroprocaine, procaine, diethanolamine,N-benzylphenethylamine, piperazine, tetramethylammonium, andtris(hydroxymethyl)aminomethane; and salts with an amino acid, such asglycine, lysine, arginine, ornithine, glutamic acid or aspartic acid.

Also, when a compound of the present invention is allowed to stand inthe air, it may absorb water to form a hydrate. Such hydrates also forma part of the present invention.

Where a compound of the present invention contains an asymmetric carbonatom in its molecule, it can form optical isomers which are in the R- orS-configuration. Although these are all represented herein by a singlemolecular formula, the present invention includes both the individual,isolated isomers and mixtures, including racemates thereof. Wherestereospecific synthesis techniques are employed or optically activecompounds are employed as starting materials, individual isomers may beprepared directly; on the other hand, if a mixture of isomers isprepared, the individual isomers may be obtained by conventionalresolution techniques.

Of the compounds of the present invention, we prefer those compounds offormula (I) and salts thereof in which:

(A) one of m and n is 0, and the other is 0 or 1;

(B) k is 0 or an integer of from 1 to 8;

(C) R¹ represents a hydroxy group, an alkoxy group having from 1 to 5carbon atoms, a heterocyclic group, an alkyl group having from 1 to 12carbon atoms which is unsubstituted or is substituted by from 1 to 3substitutents selected from the group consisting of substituents α andsubstitutents γ or such a substituted or unsubstituted alkyl group inwhich the carbon chain is interrupted by an oxygen atom and/or a sulfuratom;

(D) A is a group of formula --CO--, --CON(R²)SO₂ --, --N(R²)CO--,--N(R²)CS--, --CON(R²)CO--, --N(R²)COCO-- or --N(R²)SO₂ -- [wherein, R²is a hydrogen atom, an alkyl group having from 1 to 12 carbon atoms or abenzyl group], in particular a group of formula --CON(R²)SO₂ --,--N(R²)CS--, --CON(R²)CO--, --N(R²)COCO--, or --N(R²)SO₂ --;

(E) B represents a single bond, or a group of formula --N(R⁵)-- or--N(R⁵)N(R⁶)-- [wherein R⁵ and R⁶ are the same or different and eachrepresents a hydrogen atom, an alkyl group having from 1 to 12 carbonatoms or a benzyl group];

Of the above, we particularly prefer those compounds of formula (I) inwhich m and n are as defined in (A) above, k is as defined in (B) above,R¹ is as defined in (C) above, A is as defined in (D) above, and B is asdefined in (E) above.

More preferred compounds of the present invention are those compounds offormula (I) and salts thereof in which:

(F) both of m and n are 0;

(G) k is an integer of from 2 to 6;

(H) R¹ represents an alkyl group having from 1 to 5 carbon atoms, analkoxycarbonylalkyl group having from 3 to 8 carbon atoms, acarboxyalkyl group having from 2 to 7 carbon atoms, a hydroxyalkyl grouphaving from 2 to 5 carbon atoms, a heterocyclic group, an alkoxy grouphaving from 1 to 5 carbon atoms or hydroxy group;

(I) A represents a group of formula --CO--, --CON(R²)SO₂ --,--N(R²)CO--, --N(R²)CS--, --CON(R²)CO--, --N(R²)COCO-- or --N(R²)SO₂ --[wherein R² represents a hydrogen atom or an alkyl group having from 1to 12 carbon atoms], in particular a group of formula --CON(R²)SO₂ --,--N(R²)CS--, --CON(R²)CO--, --N(R²)COCO--, or --N(R²)SO₂ --;

(J) B represents a single bond, or a group of formula --N(R⁵)-- or--N(R⁵)N(R⁶)-- [wherein R⁵ and R⁶ are the same or different and eachrepresents a hydrogen atom or an alkyl group having from 1 to 12 carbonatoms];

Of the above, we particularly prefer those compounds of formula (I) inwhich m and n are as defined in (F) above, k is as defined in (G) above,R¹ is as defined in (H) above, A is as defined in (I) above, and B is asdefined in (J) above.

The most preferred compounds of the present invention are thosecompounds of formula (I) and salts thereof in which:

(K) both of m and n are 0;

(L) k is 4 or 5;

(M) R¹ represents an alkyl group having from 1 to 5 carbon atoms, analkoxycarbonylalkyl group having from 3 to 8 carbon atoms, acarboxyalkyl group having from 2 to 7 carbon atoms, a hydroxyalkyl grouphaving from 2 to 5 carbon atoms, a heterocyclic group or an alkoxy grouphaving from 1 to 5 carbon atoms;

(N) A represents a group of formula --CONHSO₂ --, --CONCH₃ SO₂ --,--NHCO--, --NHCS--, --CONHCO--, --NHCOCO--, --NHSO₂ -- or --CO--, inparticular a group of formula --CONHSO₂ --, --CONCH₃ SO₂ --, --NHCS--,--CONHCO--, --NHCOCO--, or --NHSO₂ --;

(O) B represents a single bond, or a group of formula --NH--, --NCH₃ --or --NHNCH₃ --;

Of the above, we particularly prefer those compounds of formula (I) inwhich m and n are as defined in (K) above, k is as defined in (L) above,R¹ is as defined in (M) above, A is as defined in (N) above, and B is asdefined in (O) above.

Specific examples of individual compounds of the present invention areshown in the following formulae (I-1), (I-2) and (I-3), in which thesubstituent groups are as shown in the corresponding one of Tables 1 to3. In the Tables, the following abbreviations are used:

    ______________________________________                                        Ac                 acetyl;                                                      Bu butyl;                                                                     iBu isobutyl;                                                                 sBu sec-butyl;                                                                tBu t-butyl;                                                                  Bz benzyl;                                                                    1,3-diox-IInd isoindol-1,3-dione-2-yl;                                        3,4-diMe-2,5-diox-1-Imdd 3,4-dimethyl-imidazolidin-                            2,5-dione-lyl,                                                               Et ethyl;                                                                     Hx hexyl;                                                                     Indn indolinyl;                                                               Me methyl;                                                                    Mor morpholino;                                                               Ph phenyl;                                                                    Pipra piperazino;                                                             Pipri piperidino;                                                             Pn pentyl;                                                                    ipn isopentyl;                                                                Pr propyl;                                                                    iPr isopropyl;                                                                Py pyridyl;                                                                   Pyr pyrrolidinyl;                                                             Thiad 3-thiazolidinyl;                                                        Thmor thiomorpholino.                                                       ______________________________________                                    

Also, in the Tables, the groups represented by Z-1 to Z-12 have thefollowing formulae: ##STR5##

                                      TABLE 1                                     __________________________________________________________________________    Cpd.                                                                            No. k A B R.sup.1                                                           __________________________________________________________________________    1-1 4   CO         NH     H                                                     1-2 4 CO NH Ph                                                                1-3 4 CO NH 2-Me--Ph                                                          1-4 4 CO NH 4-Me--Ph                                                          1-5 4 CO NH 2,4-diMe--Ph                                                      1-6 4 CO NH 3,4-diMe--Ph                                                      1-7 4 CO NH 2-(CF.sub.3)Ph                                                    1-8 4 CO NH 4-(CF.sub.3)Ph                                                    1-9 4 CO NH 2-MeOPh                                                           1-10 4 CO NH 4-MeOPh                                                          1-11 4 CO NH 2-EtOPh                                                          1-12 4 CO NH 4-EtOPh                                                          1-13 4 CO NH 2-HOPh                                                           1-14 4 CO NH 4-HOPh                                                           1-15 4 CO NH 2-(HOOC)Ph                                                       1-16 4 CO NH 4-(HOOC)Ph                                                       1-17 4 CO NH 2-(MeOOC)Ph                                                      1-18 4 CO NH 4-(MeOOC)Ph                                                      1-19 4 CO NH 2-(EtOOC)Ph                                                      1-20 4 CO NH 4-(EtOOC)Ph                                                      1-21 4 CO NH 2-(tBuOOC)Ph                                                     1-22 4 CO NH 4-(tBuOOC)Ph                                                     1-23 4 CO NH 2-Cl--Ph                                                         1-24 4 CO NH 4-Cl--Ph                                                         1-25 4 CO NH 2-Br--Ph                                                         1-26 4 CO NH 4-Br--Ph                                                         1-27 4 CO NH 2-I--Ph                                                          1-28 4 CO NH 4-I--Ph                                                          1-29 4 CO NH 2-NO.sub.2 --Ph                                                  1-30 4 CO NH 4-NO.sub.2 --Ph                                                  1-31 4 CO NH 2-NH.sub.2 --Ph                                                  1-32 4 CO NH 4-NH.sub.2 --Ph                                                  1-33 4 CO NH 2-(HO.sub.3 S)Ph                                                 1-34 4 CO NH 4-(HO.sub.3 S)Ph                                                 1-35 4 CO NH 2-(NH.sub.2 O.sub.2 S)Ph                                         1-36 4 CO NH 4-(NH.sub.2 O.sub.2 S)Ph                                         1-37 4 CO NH 2-CN--Ph                                                         1-38 4 CO NH 4-CN--Ph                                                         1-39 4 CO NH 2-(HOCH.sub.2)Ph                                                 1-40 4 CO NH 4-(HOCH.sub.2)Ph                                                 1-41 4 CO NH Me                                                               1-42 4 CO NH Et                                                               1-43 4 CO NH Pr                                                               1-44 4 CO NH iPr                                                              1-45 4 CO NH Bu                                                               1-46 4 CO NH HOOCCH.sub.2 --                                                  1-47 4 CO NH MeOOCCH.sub.2 --                                                 1-48 4 CO NH MeCH(COOH)--                                                     1-49 4 CO NH HOOC--(CH.sub.2).sub.2 --                                        1-50 4 CO NH MeCH(COOMe)--                                                    1-51 4 CO NH 1-HOOC-iBu                                                       1-52 4 CO NH 1-MeOOC-iBu                                                      1-53 4 CO NH 1-HOOC-iPn                                                       1-54 4 CO NH 1-MeOOC-iPn                                                      1-55 4 CO NH 1-HOOC-2-Me--Bu                                                  1-56 4 CO NH 1-MeOOC-2-Me--Bu                                                 1-57 4 CO NH CH.sub.2 CH.sub.2 SO.sub.3 H                                     1-58 4 CO NH OH                                                               1-59 4 CO NH MeO                                                              1-60 4 CO NH EtO                                                              1-61 4 CO NH PrO                                                              1-62 4 CO NH iPrO                                                             1-63 4 CO NH BuO                                                              1-64 4 CO NH iBuO                                                             1-65 4 CO NH sBuO                                                             1-66 4 CO NH tBuO                                                             1-67 4 CO NH HxO                                                              1-68 4 CO NH PhO                                                              1-69 4 CO NH BzO                                                              1-70 4 CO NH Z-1                                                              1-71 4 CO NH Z-2                                                              1-72 4 CO NH Z-3                                                              1-73 4 CO NH Z-4                                                              1-74 4 CO NH Z-5                                                              1-75 4 CO NH Z-6                                                              1-76 4 CO NH Z-7                                                              1-77 4 CO NH Z-8                                                              1-78 4 CO NH Z-9                                                              1-79 4 CO NH Z-10                                                             1-80 4 CO NH Z-11                                                             1-81 4 CO NH Z-12                                                             1-82 4 CO NH 3-Py                                                             1-83 4 CO NH 4-Py                                                             1-84 4 CO N(Ac) H                                                             1-85 4 CO N(Ac) Ph                                                            1-86 4 CO N(Ac) 2-Me--Ph                                                      1-87 4 CO N(Ac) 4-Me--Ph                                                      1-88 4 CO N(Ac) 2,4-diMe--Ph                                                  1-89 4 CO N(Ac) 3,4-diMe--Ph                                                  1-90 4 CO N(Ac) 2-(CF.sub.3)Ph                                                1-91 4 CO N(Ac) 4-(CF.sub.3)Ph                                                1-92 4 CO N(Ac) 2-MeOPh                                                       1-93 4 CO N(Ac) 4-MeOPh                                                       1-94 4 CO N(Ac) 2-EtOPh                                                       1-95 4 CO N(Ac) 4-EtOPh                                                       1-96 4 CO N(Ac) 2-HOPh                                                        1-97 4 CO N(Ac) 4-HOPh                                                        1-98 4 CO N(Ac) 2-(HOOC)Ph                                                    1-99 4 CO N(Ac) 4-(HOOC)Ph                                                    1-100 4 CO N(Ac) 2-(MeOOC)Ph                                                  1-101 4 CO N(Ac) 4-(MeOOC)Ph                                                  1-102 4 CO N(Ac) 2-(EtOOC)Ph                                                  1-103 4 CO N(Ac) 4-(EtOOC)Ph                                                  1-104 4 CO N(Ac) 2-(tBuOOC)Ph                                                 1-105 4 CO N(Ac) 4-(tBuOOC)Ph                                                 1-106 4 CO N(Ac) 2-Cl--Ph                                                     1-107 4 CO N(Ac) 4-Cl--Ph                                                     1-108 4 CO N(Ac) 2-Br--Ph                                                     1-109 4 CO N(Ac) 4-Br--Ph                                                     1-110 4 CO N(Ac) 2-I--Ph                                                      1-111 4 CO N(Ac) 4-I--Ph                                                      1-112 4 CO N(Ac) 2-NO.sub.2 --Ph                                              1-113 4 CO N(Ac) 4-NO.sub.2 --Ph                                              1-114 4 CO N(Ac) 2-NH.sub.2 --Ph                                              1-115 4 CO N(Ac) 4-NH.sub.2 --Ph                                              1-116 4 CO N(Ac) 2-(HO.sub.3 S)Ph                                             1-117 4 CO N(Ac) 4-(HO.sub.3 S)Ph                                             1-118 4 CO N(Ac) 2-(NH.sub.2 O.sub.2 S)Ph                                     1-119 4 CO N(Ac) 4-(NH.sub.2 O.sub.2 S)Ph                                     1-120 4 CO N(Ac) 2-CN--Ph                                                     1-121 4 CO N(Ac) 4-CN--Ph                                                     1-122 4 CO N(Ac) 2-(HOCH.sub.2)Ph                                             1-123 4 CO N(Ac) 4-(HOCH.sub.2)Ph                                             1-124 4 CO N(Ac) Me                                                           1-125 4 CO N(Ac) Et                                                           1-126 4 CO N(Ac) Pr                                                           1-127 4 CO N(Ac) iPr                                                          1-128 4 CO N(Ac) Bu                                                           1-129 4 CO N(Ac) HOOCCH.sub.2 --                                              1-130 4 CO N(Ac) MeOOCCH.sub.2 --                                             1-131 4 CO N(Ac) MeCH(COOH)                                                   1-132 4 CO N(Ac) HOOC--(CH.sub.2).sub.2 --                                    1-133 4 CO N(Ac) MeCH(COOMe)                                                  1-134 4 CO N(Ac) 1-HOOC-iBu                                                   1-135 4 CO N(Ac) 1-MeOOC-iBu                                                  1-136 4 CO N(Ac) 1-HOOC-iPn                                                   1-137 4 CO N(Ac) 1-MeOOC-iPn                                                  1-138 4 CO N(Ac) 1-HOOC-2-Me--Bu                                              1-139 4 CO N(Ac) 1-MeOOC-2-Me--Bu                                             1-140 4 CO N(Ac) CH.sub.2 CH.sub.2 SO.sub.3 H                                 1-141 4 CO N(Ac) OH                                                           1-142 4 CO N(Ac) MeO                                                          1-143 4 CO N(Ac) EtO                                                          1-144 4 CO N(Ac) PrO                                                          1-145 4 CO N(Ac) iPrO                                                         1-146 4 CO N(Ac) BuO                                                          1-147 4 CO N(Ac) iBuO                                                         1-148 4 CO N(Ac) sBuO                                                         1-149 4 CO N(Ac) tBuO                                                         1-150 4 CO N(Ac) HxO                                                          1-151 4 CO N(Ac) PhO                                                          1-152 4 CO N(Ac) BzO                                                          1-153 4 CO N(Ac) Z-1                                                          1-154 4 CO N(Ac) Z-2                                                          1-155 4 CO N(Ac) Z-3                                                          1-156 4 CO N(Ac) Z-4                                                          1-157 4 CO N(Ac) Z-5                                                          1-158 4 CO N(Ac) Z-6                                                          1-159 4 CO N(Ac) Z-7                                                          1-160 4 CO N(Ac) Z-8                                                          1-161 4 CO N(Ac) Z-9                                                          1-162 4 CO N(Ac) Z-10                                                         1-163 4 CO N(Ac) Z-11                                                         1-164 4 CO N(Ac) Z-12                                                         1-165 4 CO N(Ac) 3-Py                                                         1-166 4 CO N(Ac) 4-Py                                                         1-167 4 COO -- H                                                              1-168 4 COO -- Ph                                                             1-169 4 COO -- 2-Me--Ph                                                       1-170 4 COO -- 4-Me--Ph                                                       1-171 4 COO -- 2,4-diMe--Ph                                                   1-172 4 COO -- 3,4-diMe--Ph                                                   1-173 4 COO -- 2-(CF.sub.3)Ph                                                 1-174 4 COO -- 4-(CF.sub.3)Ph                                                 1-175 4 COO -- 2-MeOPh                                                        1-176 4 COO -- 4-MeOPh                                                        1-177 4 COO -- 2-EtOPh                                                        1-178 4 COO -- 4-EtOPh                                                        1-179 4 COO -- 2-HOPh                                                         1-180 4 COO -- 4-HOPh                                                         1-181 4 COO -- 2-(HOOC)Ph                                                     1-182 4 COO -- 4-(HOOC)Ph                                                     1-183 4 COO -- 2-(MeOOC)Ph                                                    1-184 4 COO -- 4-(MeOOC)Ph                                                    1-185 4 COO -- 2-(EtOOC)Ph                                                    1-186 4 COO -- 4-(EtOOC)Ph                                                    1-187 4 COO -- 2-(tBuOOC)Ph                                                   1-188 4 COO -- 4-(tBuOOC)Ph                                                   1-189 4 COO -- 2-Cl--Ph                                                       1-190 4 COO -- 4-Cl--Ph                                                       1-191 4 COO -- 2-Br--Ph                                                       1-192 4 COO -- 4-Br--Ph                                                       1-193 4 COO -- 2-I--Ph                                                        1-194 4 COO -- 4-I--Ph                                                        1-195 4 COO -- 2-NO.sub.2 --Ph                                                1-196 4 COO -- 4-NO.sub.2 --Ph                                                1-197 4 COO -- 2-NH.sub.2 --Ph                                                1-198 4 COO -- 4-NH.sub.2 --Ph                                                1-199 4 COO -- 2-(HO.sub.3 S)Ph                                               1-200 4 COO -- 4-(HO.sub.3 S)Ph                                               1-201 4 COO -- 2-(NH.sub.2 O.sub.2 S)Ph                                       1-202 4 COO -- 4-(NH.sub.2 O.sub.2 S)Ph                                       1-203 4 COO -- 2-CN--Ph                                                       1-204 4 COO -- 4-CN--Ph                                                       1-205 4 COO -- 2-(HOCH.sub.2)Ph                                               1-206 4 COO -- 4-(HOCH.sub.2)Ph                                               1-207 4 COO -- Me                                                             1-208 4 COO -- Et                                                             1-209 4 COO -- Pr                                                             1-210 4 COO -- iPr                                                            1-211 4 COO -- Bu                                                             1-212 4 COO -- HOOCCH.sub.2 --                                                1-213 4 COO -- HOOC--(CH.sub.2).sub.2 --                                      1-214 4 COO -- MeCH(COOMe)                                                    1-215 4 COO -- 1-HOOC-iBu                                                     1-216 4 COO -- 1-HOOC-iPn                                                     1-217 4 COO -- Z-1                                                            1-218 4 COO -- Z-2                                                            1-219 4 COO -- Z-3                                                            1-220 4 COO -- Z-4                                                            1-221 4 COO -- Z-5                                                            1-222 4 COO -- Z-6                                                            1-223 4 COO -- Z-7                                                            1-224 4 COO -- Z-8                                                            1-225 4 COO -- Z-9                                                            1-226 4 COO -- Z-10                                                           1-227 4 COO -- Z-11                                                           1-228 4 COO -- Z-12                                                           1-229 4 COO -- 3-Py                                                           1-230 4 COO -- 4-Py                                                           1-231 4 CONHCO -- H                                                           1-232 4 CONHCO -- Ph                                                          1-233 4 CONHCO -- 2-Me--Ph                                                    1-234 4 CONHCO -- 4-Me--Ph                                                    1-235 4 CONHCO -- 2,4-diMe--Ph                                                1-236 4 CONHCO -- 3,4-diMe--Ph                                                1-237 4 CONHCO -- 2-(CF.sub.3)Ph                                              1-238 4 CONHCO -- 4-(CF.sub.3)Ph                                              1-239 4 CONHCO -- 2-MeOPh                                                     1-240 4 CONHCO -- 4-MeOPh                                                     1-241 4 CONHCO -- 2-EtOPh                                                     1-242 4 CONHCO -- 4-EtOPh                                                     1-243 4 CONHCO -- 2-HOPh                                                      1-244 4 CONHCO -- 4-HOPh                                                      1-245 4 CONHCO -- 2-(HOOC)Ph                                                  1-246 4 CONHCO -- 4-(HOOC)Ph                                                  1-247 4 CONHCO -- 2-(MeOOC)Ph                                                 1-248 4 CONHCO -- 4-(MeOOC)Ph                                                 1-249 4 CONHCO -- 2-(EtOOC)Ph                                                 1-250 4 CONHCO -- 4-(EtOOC)Ph                                                 1-251 4 CONHCO -- 2-(tBuOOC)Ph                                                1-252 4 CONHCO -- 4-(tBuOOC)Ph                                                1-253 4 CONHCO -- 2-Cl--Ph                                                    1-254 4 CONHCO -- 4-Cl--Ph                                                    1-255 4 CONHCO -- 2-Br--Ph                                                    1-256 4 CONHCO -- 4-Br--Ph                                                    1-257 4 CONHCO -- 2-I--Ph                                                     1-258 4 CONHCO -- 4-I--Ph                                                     1-259 4 CONHCO -- 2-NO.sub.2 --Ph                                             1-260 4 CONHCO -- 4-NO.sub.2 --Ph                                             1-261 4 CONHCO -- 2-NH.sub.2 --Ph                                             1-262 4 CONHCO -- 4-NH.sub.2 --Ph                                             1-263 4 CONHCO -- 2-(HO.sub.3 S)Ph                                            1-264 4 CONHCO -- 4-(HO.sub.3 S)Ph                                            1-265 4 CONHCO -- 2-(NH.sub.2 O.sub.2 S)Ph                                    1-266 4 CONHCO -- 4-(NH.sub.2 O.sub.2 S)Ph                                    1-267 4 CONHCO -- 2-CN--Ph                                                    1-268 4 CONHCO -- 4-CN--Ph                                                    1-269 4 CONHCO -- 2-(HOCH.sub.2)Ph                                            1-270 4 CONHCO -- 4-(HOCH.sub.2)Ph                                            1-271 4 CONHCO -- Me                                                          1-272 4 CONHCO -- Et                                                          1-273 4 CONHCO -- Pr                                                          1-274 4 CONHCO -- iPr                                                         1-275 4 CONHCO -- Bu                                                          1-276 4 CONHCO -- HOOCCH.sub.2 --                                             1-277 4 CONHCO -- MeOOCCH.sub.2 --                                            1-278 4 CONHCO -- MeCH(COOH)                                                  1-279 4 CONHCO -- HOOC--(CH.sub.2).sub.2 --                                   1-280 4 CONHCO -- MeCH(COOMe)                                                 1-281 4 CONHCO -- 1-HOOC-iBu                                                  1-282 4 CONHCO -- 1-MeOOC-iBu                                                 1-283 4 CONHCO -- 1-HOOC-iPn                                                  1-284 4 CONHCO -- 1-MeOOC-iPn                                                 1-285 4 CONHCO -- 1-HOOC-2-Me--Bu                                             1-286 4 CONHCO -- 1-MeOOC-2-Me--Bu                                            1-287 4 CONHCO -- CH.sub.2 CH.sub.2 SO.sub.3 H                                1-288 4 CONHCO -- Z-1                                                         1-289 4 CONHCO -- Z-2                                                         1-290 4 CONHCO -- Z-3                                                         1-291 4 CONHCO -- Z-4                                                         1-292 4 CONHCO -- Z-5                                                         1-293 4 CONHCO -- Z-6                                                         1-294 4 CONHCO -- Z-7                                                         1-295 4 CONHCO -- Z-8                                                         1-296 4 CONHCO -- Z-9                                                         1-297 4 CONHCO -- Z-10                                                        1-298 4 CONHCO -- Z-11                                                        1-299 4 CONHCO -- Z-12                                                        1-300 4 CONHCO -- 3-Py                                                        1-301 4 CONHCO -- 4-Py                                                        1-302 4 CON(Ac)CO -- H                                                        1-303 4 CON(Ac)CO -- Ph                                                       1-304 4 CON(Ac)CO -- 2-Me--Ph                                                 1-305 4 CON(Ac)CO -- 4-Me--Ph                                                 1-306 4 CON(Ac)CO -- 2,4-diMe--Ph                                             1-307 4 CON(Ac)CO -- 3,4-diMe--Ph                                             1-308 4 CON(Ac)CO -- 2-(CF.sub.3)Ph                                           1-309 4 CON(Ac)CO -- 4-(CF.sub.3)Ph                                           1-310 4 CON(Ac)CO -- 2-MeOPh                                                  1-311 4 CON(Ac)CO -- 4-MeOPh                                                  1-312 4 CON(Ac)CO -- 2-EtOPh                                                  1-313 4 CON(Ac)CO -- 4-EtOPh                                                  1-314 4 CON(Ac)CO -- 2-HOPh                                                   1-315 4 CON(Ac)CO -- 4-HOPh                                                   1-316 4 CON(Ac)CO -- 2-(HOOC)Ph                                               1-317 4 CON(Ac)CO -- 4-(HOOC)Ph                                               1-318 4 CON(Ac)CO -- 2-(MeOOC)Ph                                              1-319 4 CON(Ac)CO -- 4-(MeOOC)Ph                                              1-320 4 CON(Ac)CO -- 2-(EtOOC)Ph                                              1-321 4 CON(Ac)CO -- 4-(EtOOC)Ph                                              1-322 4 CON(Ac)CO -- 2-(tBuOOC)Ph                                             1-323 4 CON(Ac)CO -- 4-(tBuOOC)Ph                                             1-324 4 CON(Ac)CO -- 2-Cl--Ph                                                 1-325 4 CON(Ac)CO -- 4-Cl--Ph                                                 1-326 4 CON(Ac)CO -- 2-Br--Ph                                                 1-327 4 CON(Ac)CO -- 4-Br--Ph                                                 1-328 4 CON(Ac)CO -- 2-I--Ph                                                  1-329 4 CON(Ac)CO -- 4-I--Ph                                                  1-330 4 CON(Ac)CO -- 2-NO.sub.2 --Ph                                          1-331 4 CON(Ac)CO -- 4-NO.sub.2 --Ph                                          1-332 4 CON(Ac)CO -- 2-NH.sub.2 --Ph                                          1-333 4 CON(Ac)CO -- 4-NH.sub.2 --Ph                                          1-334 4 CON(Ac)CO -- 2-(HO.sub.3 S)Ph                                         1-335 4 CON(Ac)CO -- 4-(HO.sub.3 S)Ph                                         1-336 4 CON(Ac)CO -- 2-(NH.sub.2 O.sub.2 S)Ph                                 1-337 4 CON(Ac)CO -- 4-(NH.sub.2 O.sub.2 S)Ph                                 1-338 4 CON(Ac)CO -- 2-CN--Ph                                                 1-339 4 CON(Ac)CO -- 4-CN--Ph                                                 1-340 4 CON(Ac)CO -- 2-(HOCH.sub.2)Ph                                         1-341 4 CON(Ac)CO -- 4-(HOCH.sub.2)Ph                                         1-342 4 CON(Ac)CO -- Me                                                       1-343 4 CON(Ac)CO -- Et                                                       1-344 4 CON(Ac)CO -- Pr                                                       1-345 4 CON(Ac)CO -- iPr                                                      1-346 4 CON(Ac)CO -- Bu                                                       1-347 4 CON(Ac)CO -- HOOCCH.sub.2 --                                          1-348 4 CON(Ac)CO -- MeOOCCH.sub.2 --                                         1-349 4 CON(Ac)CO -- MeCH(COOH)                                               1-350 4 CON(Ac)CO -- HOOC--(CH.sub.2).sub.2 --                                1-351 4 CON(Ac)CO -- MeCH(COOMe)                                              1-352 4 CON(Ac)CO -- 1-HOOC-iBu                                               1-353 4 CON(Ac)CO -- 1-MeOOC-iBu                                              1-354 4 CON(Ac)CO -- 1-HOOC-iPn                                               1-355 4 CON(Ac)CO -- 1-MeOOC-iPn                                              1-356 4 CON(Ac)CO -- 1-HOOC-2-Me--Bu                                          1-357 4 CON(Ac)CO -- 1-MeOOC-2-Me--Bu                                         1-358 4 CON(Ac)CO -- CH.sub.2 CH.sub.2 SO.sub.3 H                             1-359 4 CON(Ac)CO -- Z-1                                                      1-360 4 CON(Ac)CO -- Z-2                                                      1-361 4 CON(Ac)CO -- Z-3                                                      1-362 4 CON(Ac)CO -- Z-4                                                      1-363 4 CON(Ac)CO -- Z-5                                                      1-364 4 CON(Ac)CO -- Z-6                                                      1-365 4 CON(Ac)CO -- Z-7                                                      1-366 4 CON(Ac)CO -- Z-8                                                      1-367 4 CON(Ac)CO -- Z-9                                                      1-368 4 CON(Ac)CO -- Z-10                                                     1-369 4 CON(Ac)CO -- Z-11                                                     1-370 4 CON(Ac)CO -- Z-12                                                     1-371 4 CON(Ac)CO -- 3-Py                                                     1-372 4 CON(Ac)CO -- 4-Py                                                     1-373 4 CONHCO NH H                                                           1-374 4 CONHCO NH Ph                                                          1-375 4 CONHCO NH 2-Me--Ph                                                    1-376 4 CONHCO NH 4-Me--Ph                                                    1-377 4 CONHCO NH 2,4-diMe--Ph                                                1-378 4 CONHCO NH 3,4-diMe--Ph                                                1-379 4 CONHCO NH 2-(CF.sub.3)Ph                                              1-380 4 CONHCO NH 4-(CF.sub.3)Ph                                              1-381 4 CONHCO NH 2-MeOPh                                                     1-382 4 CONHCO NH 4-MeOPh                                                     1-383 4 CONHCO NH 2-EtOPh                                                     1-384 4 CONHCO NH 4-EtOPh                                                     1-385 4 CONHCO NH 2-HOPh                                                      1-386 4 CONHCO NH 4-HOPh                                                      1-387 4 CONHCO NH 2-(HOOC)Ph                                                  1-388 4 CONHCO NH 4-(HOOC)Ph                                                  1-389 4 CONHCO NH 2-(MeOOC)Ph                                                 1-390 4 CONHCO NH 4-(MeOOC)Ph                                                 1-391 4 CONHCO NH 2-(EtOOC)Ph                                                 1-392 4 CONHCO NH 4-(EtOOC)Ph                                                 1-393 4 CONHCO NH 2-(tBuOOC)Ph                                                1-394 4 CONHCO NH 4-(tBuOOC)Ph                                                1-395 4 CONHCO NH 2-Cl--Ph                                                    1-396 4 CONHCO NH 4-Cl--Ph                                                    1-397 4 CONHCO NH 2-Br--Ph                                                    1-398 4 CONHCO NH 4-Br--Ph                                                    1-399 4 CONHCO NH 2-I--Ph                                                     1-400 4 CONHCO NH 4-I--Ph                                                     1-401 4 CONHCO NH 2-NO.sub.2 --Ph                                             1-402 4 CONHCO NH 4-NO.sub.2 --Ph                                             1-403 4 CONHCO NH 2-NH.sub.2 --Ph                                             1-404 4 CONHCO NH 4-NH.sub.2 --Ph                                             1-405 4 CONHCO NH 2-(HO.sub.3 S)Ph                                            1-406 4 CONHCO NH 4-(HO.sub.3 S)Ph                                            1-407 4 CONHCO NH 2-(NH.sub.2 O.sub.2 S)Ph                                    1-408 4 CONHCO NH 4-(NH.sub.2 O.sub.2 S)Ph                                    1-409 4 CONHCO NH 2-CN--Ph                                                    1-410 4 CONHCO NH 4-CN--Ph                                                    1-411 4 CONHCO NH 2-(HOCH.sub.2)Ph                                            1-412 4 CONHCO NH 4-(HOCH.sub.2)Ph                                            1-413 4 CONHCO NH Me                                                          1-414 4 CONHCO NH Et                                                          1-415 4 CONHCO NH Pr                                                          1-416 4 CONHCO NH iPr                                                         1-417 4 CONHCO NH Bu                                                          1-418 4 CONHCO NH HOOCCH.sub.2 --                                             1-419 4 CONHCO NH MeOOCCH.sub.2 --                                            1-420 4 CONHCO NH MeCH(COOH)                                                  1-421 4 CONHCO NH HOOC-(CH.sub.2).sub.2 --                                    1-422 4 CONHCO NH MeCH(COOMe)                                                 1-423 4 CONHCO NH 1-HOOC-iBu                                                  1-424 4 CONHCO NH 1-MeOOC-iBu                                                 1-425 4 CONHCO NH 1-HOOC-iPn                                                  1-426 4 CONHCO NH 1-MeOOC-iPn                                                 1-427 4 CONHCO NH 1-HOOC-2-Me--Bu                                             1-428 4 CONHCO NH 1-MeOOC-2-Me--Bu                                            1-429 4 CONHCO NH CH.sub.2 CH.sub.2 SO.sub.3 H                                1-430 4 CONHCO NH HO                                                          1-431 4 CONHCO NH MeO                                                         1-432 4 CONHCO NH EtO                                                         1-433 4 CONHCO NH PrO                                                         1-434 4 CONHCO NH iPrO                                                        1-435 4 CONHCO NH BuO                                                         1-436 4 CONHCO NH iBuO                                                        1-437 4 CONHCO NH sBuO                                                        1-438 4 CONHCO NH tBuO                                                        1-439 4 CONHCO NH HxO                                                         1-440 4 CONHCO NH PhO                                                         1-441 4 CONHCO NH BzO                                                         1-442 4 CONHCO NH Z-1                                                         1-443 4 CONHCO NH Z-2                                                         1-444 4 CONHCO NH Z-3                                                         1-445 4 CONHCO NH Z-4                                                         1-446 4 CONHCO NH Z-5                                                         1-447 4 CONHCO NH Z-6                                                         1-448 4 CONHCO NH Z-7                                                         1-449 4 CONHCO NH Z-8                                                         1-450 4 CONHCO NH Z-9                                                         1-451 4 CONHCO NH Z-10                                                        1-452 4 CONHCO NH Z-11                                                        1-453 4 CONHCO NH Z-12                                                        1-454 4 CONHCO NH 3-Py                                                        1-455 4 CONHCO NH 4-Py                                                        1-456 4 CONHSO.sub.2 -- H                                                     1-457 4 CONHSO.sub.2 -- Ph                                                    1-458 4 CONHSO.sub.2 -- 2-Me--Ph                                              1-459 4 CONHSO.sub.2 -- 4-Me--Ph                                              1-460 4 CONHSO.sub.2 -- 2,4-diMe--Ph                                          1-461 4 CONHSO.sub.2 -- 3,4-diMe--Ph                                          1-462 4 CONHSO.sub.2 -- 2-(CF.sub.3)Ph                                        1-463 4 CONHSO.sub.2 -- 4-(CF.sub.3)Ph                                        1-464 4 CONHSO.sub.2 -- 2-MeOPh                                               1-465 4 CONHSO.sub.2 -- 4-MeOPh                                               1-466 4 CONHSO.sub.2 -- 2-EtOPh                                               1-467 4 CONHSO.sub.2 -- 4-EtOPh                                               1-468 4 CONHSO.sub.2 -- 2-HOPh                                                1-469 4 CONHSO.sub.2 -- 4-HOPh                                                1-470 4 CONHSO.sub.2 -- 2-(HOOC)Ph                                            1-471 4 CONHSO.sub.2 -- 4-(HOOC)Ph                                            1-472 4 CONHSO.sub.2 -- 2-(MeOOC)Ph                                           1-473 4 CONHSO.sub.2 -- 4-(MeOOC)Ph                                           1-474 4 CONHSO.sub.2 -- 2-(EtOOC)Ph                                           1-475 4 CONHSO.sub.2 -- 4-(EtOOC)Ph                                           1-476 4 CONHSO.sub.2 -- 2-(tBuOOC)Ph                                          1-477 4 CONHSO.sub.2 -- 4-(tBuOOC)Ph                                          1-478 4 CONHSO.sub.2 -- 2-Cl--Ph                                              1-479 4 CONHSO.sub.2 -- 4-Cl--Ph                                              1-480 4 CONHSO.sub.2 -- 2-Br--Ph                                              1-481 4 CONHSO.sub.2 -- 4-Br--Ph                                              1-482 4 CONHSO.sub.2 -- 2-I--Ph                                               1-483 4 CONHSO.sub.2 -- 4-I--Ph                                               1-484 4 CONHSO.sub.2 -- 2-NO.sub.2 --Ph                                       1-485 4 CONHSO.sub.2 -- 4-NO.sub.2 --Ph                                       1-486 4 CONHSO.sub.2 -- 2-NH.sub.2 --Ph                                       1-487 4 CONHSO.sub.2 -- 4-NH.sub.2 --Ph                                       1-488 4 CONHSO.sub.2 -- 2-(HO.sub.3 S)Ph                                      1-489 4 CONHSO.sub.2 -- 4-(HO.sub.3 S)Ph                                      1-490 4 CONHSO.sub.2 -- 2-(NH.sub.2 O.sub.2 S)Ph                              1-491 4 CONHSO.sub.2 -- 4-(NH.sub.2 O.sub.2 S)Ph                              1-492 4 CONHSO.sub.2 -- 2-CN--Ph                                              1-493 4 CONHSO.sub.2 -- 4-CN--Ph                                              1-494 4 CONHSO.sub.2 -- 2-(HOCH.sub.2)Ph                                      1-495 4 CONHSO.sub.2 -- 4-(HOCH.sub.2)Ph                                      1-496 4 CONHSO.sub.2 -- Me                                                    1-497 4 CONHSO.sub.2 -- Et                                                    1-498 4 CONHSO.sub.2 -- Pr                                                    1-499 4 CONHSO.sub.2 -- iPr                                                   1-500 4 CONHSO.sub.2 -- Bu                                                    1-501 4 CONHSO.sub.2 -- HOOCCH.sub.2 --                                       1-502 4 CONHSO.sub.2 -- MeOOCCH.sub.2 --                                      1-503 4 CONHSO.sub.2 -- MeCH(COOH)                                            1-504 4 CONHSO.sub.2 -- HOOC--(CH.sub.2).sub.2 --                             1-505 4 CONHSO.sub.2 -- MeCH(COOMe)                                           1-506 4 CONHSO.sub.2 -- 1-HOOC-iBu                                            1-507 4 CONHSO.sub.2 -- 1-MeOOC-iBu                                           1-508 4 CONHSO.sub.2 -- 1-HOOC-iPn                                            1-509 4 CONHSO.sub.2 -- 1-MeOOC-iPn                                           1-510 4 CONHSO.sub.2 -- 1-HOOC-2-Me--Bu                                       1-511 4 CONHSO.sub.2 -- 1-MeOOC-2-Me--Bu                                      1-512 4 CONHSO.sub.2 -- CH.sub.2 CH.sub.2 SO.sub.3 H                          1-513 4 CONHSO.sub.2 -- OH                                                    1-514 4 CONHSO.sub.2 -- MeO                                                   1-515 4 CONHSO.sub.2 -- EtO                                                   1-516 4 CONHSO.sub.2 -- PrO                                                   1-517 4 CONHSO.sub.2 -- iPrO                                                  1-518 4 CONHSO.sub.2 -- BuO                                                   1-519 4 CONHSO.sub.2 -- iBuO                                                  1-520 4 CONHSO.sub.2 -- sBuO                                                  1-521 4 CONHSO.sub.2 -- tBuO                                                  1-522 4 CONHSO.sub.2 -- HxO                                                   1-523 4 CONHSO.sub.2 -- PhO                                                   1-524 4 CONHSO.sub.2 -- BzO                                                   1-525 4 CONHSO.sub.2 -- Z-1                                                   1-526 4 CONHSO.sub.2 -- Z-2                                                   1-527 4 CONHSO.sub.2 -- Z-3                                                   1-528 4 CONHSO.sub.2 -- Z-4                                                   1-529 4 CONHSO.sub.2 -- Z-5                                                   1-530 4 CONHSO.sub.2 -- Z-6                                                   1-531 4 CONHSO.sub.2 -- Z-7                                                   1-532 4 CONHSO.sub.2 -- Z-8                                                   1-533 4 CONHSO.sub.2 -- Z-9                                                   1-534 4 CONHSO.sub.2 -- Z-10                                                  1-535 4 CONHSO.sub.2 -- Z-11                                                  1-536 4 CONHSO.sub.2 -- Z-12                                                  1-537 4 CONHSO.sub.2 -- 3-Py                                                  1-538 4 CONHSO.sub.2 -- 4-Py                                                  1-539 4 CONHSO.sub.2 NH H                                                     1-540 4 CONHSO.sub.2 NH Ph                                                    1-541 4 CONHSO.sub.2 NH 2-Me--Ph                                              1-542 4 CONHSO.sub.2 NH 4-Me--Ph                                              1-543 4 CONHSO.sub.2 NH 2,4-diMe--Ph                                          1-544 4 CONHSO.sub.2 NH 3,4-diMe--Ph                                          1-545 4 CONHSO.sub.2 NH 2-(CF.sub.3)Ph                                        1-546 4 CONHSO.sub.2 NH 4-(CF.sub.3)Ph                                        1-547 4 CONHSO.sub.2 NH 2-MeOPh                                               1-548 4 CONHSO.sub.2 NH 4-MeOPh                                               1-549 4 CONHSO.sub.2 NH 2-EtOPh                                               1-550 4 CONHSO.sub.2 NH 4-EtOPh                                               1-551 4 CONHSO.sub.2 NH 2-HOPh                                                1-552 4 CONHSO.sub.2 NH 4-HOPh                                                1-553 4 CONHSO.sub.2 NH 2-(HOOC)Ph                                            1-554 4 CONHSO.sub.2 NH 4-(HOOC)Ph                                            1-555 4 CONHSO.sub.2 NH 2-(MeOOC)Ph                                           1-556 4 CONHSO.sub.2 NH 4-(MeOOC)Ph                                           1-557 4 CONHSO.sub.2 NH 2-(EtOOC)Ph                                           1-558 4 CONHSO.sub.2 NH 4-(EtOOC)Ph                                           1-559 4 CONHSO.sub.2 NH 2-(tBuOOC)Ph                                          1-560 4 CONHSO.sub.2 NH 4-(tBuOOC)Ph                                          1-561 4 CONHSO.sub.2 NH 2-Cl--Ph                                              1-562 4 CONHSO.sub.2 NH 4-Cl--Ph                                              1-563 4 CONHSO.sub.2 NH 2-Br--Ph                                              1-564 4 CONHSO.sub.2 NH 4-Br--Ph                                              1-565 4 CONHSO.sub.2 NH 2-I--Ph                                               1-566 4 CONHSO.sub.2 NH 4-I--Ph                                               1-567 4 CONHSO.sub.2 NH 2-NO.sub.2 --Ph                                       1-568 4 CONHSO.sub.2 NH 4-NO.sub.2 --Ph                                       1-569 4 CONHSO.sub.2 NH 2-NH.sub.2 --Ph                                       1-570 4 CONHSO.sub.2 NH 4-NH.sub.2 --Ph                                       1-571 4 CONHSO.sub.2 NH 2-(HO.sub.3 S)Ph                                      1-572 4 CONHSO.sub.2 NH 4-(HO.sub.3 S)Ph                                      1-573 4 CONHSO.sub.2 NH 2-(NH.sub.2 O.sub.2 S)Ph                              1-574 4 CONHSO.sub.2 NH 4-(NH.sub.2 O.sub.2 S)Ph                              1-575 4 CONHSO.sub.2 NH 2-CN--Ph                                              1-576 4 CONHSO.sub.2 NH 4-CN--Ph                                              1-577 4 CONHSO.sub.2 NH 2-(HOCH.sub.2)Ph                                      1-578 4 CONHSO.sub.2 NH 4-(HOCH.sub.2)Ph                                      1-579 4 CONHSO.sub.2 NH Me                                                    1-580 4 CONHSO.sub.2 NH Et                                                    1-581 4 CONHSO.sub.2 NH Pr                                                    1-582 4 CONHSO.sub.2 NH iPr                                                   1-583 4 CONHSO.sub.2 NH Bu                                                    1-584 4 CONHSO.sub.2 NH HOOCCH.sub.2 --                                       1-555 4 CONHSO.sub.2 NH MeOOCCH.sub.2 --                                      1-586 4 CONHSO.sub.2 NH MeCH(COOH)                                            1-587 4 CONHSO.sub.2 NH HOOC--(CH.sub.2).sub.2 --                             1-588 4 CONHSO.sub.2 NH MeCH(COOMe)                                           1-589 4 CONHSO.sub.2 NH 1-HOOC-iBu                                            1-590 4 CONHSO.sub.2 NH 1-MeOOC-iBu                                           1-591 4 CONHSO.sub.2 NH 1-HOOC-iPn                                            1-592 4 CONHSO.sub.2 NH 1-MeOOC-iPn                                           1-593 4 CONHSO.sub.2 NH 1-HOOC-2-Me--Bu                                       1-594 4 CONHSO.sub.2 NH 1-MeOOC-2-Me--Bu                                      1-595 4 C0NHSO.sub.2 NH CH.sub.2 CH.sub.2 SO.sub.3 H                          1-596 4 CONHSO.sub.2 NH OH                                                    1-597 4 CONHSO.sub.2 NH MeO                                                   1-598 4 CONHSO.sub.2 NH EtO                                                   1-599 4 CONHSO.sub.2 NH PrO                                                   1-600 4 CONHSO.sub.2 NH iPrO                                                  1-601 4 CONHSO.sub.2 NH BuO                                                   1-602 4 CONHSO.sub.2 NH iBuO                                                  1-603 4 CONHSO.sub.2 NH sBuO                                                  1-604 4 CONHSO.sub.2 NH tBuO                                                  1-605 4 CONHSO.sub.2 NH HxO                                                   1-606 4 CONHSO.sub.2 NH PhO                                                   1-607 4 CONHSO.sub.2 NH BzO                                                   1-608 4 CONHSO.sub.2 NH Z-1                                                   1-609 4 CONHSO.sub.2 NH Z-2                                                   1-610 4 CONHSO.sub.2 NH Z-3                                                   1-611 4 CONHSO.sub.2 NH Z-4                                                   1-612 4 CONHSO.sub.2 NH Z-5                                                   1-613 4 CONHSO.sub.2 NH Z-6                                                   1-614 4 CONHSO.sub.2 NH Z-7                                                   1-615 4 CONHSO.sub.2 NH Z-8                                                   1-616 4 CONHSO.sub.2 NH Z-9                                                   1-617 4 CONHSO.sub.2 NH Z-10                                                  1-618 4 CONHSO.sub.2 NH Z-11                                                  1-619 4 CONHSO.sub.2 NH Z-12                                                  1-620 4 CONHSO.sub.2 NH 3-Py                                                  1-621 4 CONHSO.sub.2 NH 4-Py                                                  1-622 4 NHCO -- H                                                             1-623 4 NHCO -- Ph                                                            1-624 4 NHCO -- 2-Me--Ph                                                      1-625 4 NHCO -- 4-Me--Ph                                                      1-626 4 NHCO -- 2,4-diMe--Ph                                                  1-627 4 NHCO -- 3,4-diMe--Ph                                                  1-628 4 NHCO -- 2-(CF.sub.3)Ph                                                1-629 4 NHCO -- 4-(CF.sub.3)Ph                                                1-630 4 NHCO -- 2-MeOPh                                                       1-631 4 NHCO -- 4-MeOPh                                                       1-632 4 NHCO -- 2-EtOPh                                                       1-633 4 NHCO -- 4-EtOPh                                                       1-634 4 NHCO -- 2-HOPh                                                        1-635 4 NHCO -- 4-HOPh                                                        1-636 4 NHCO -- 2-(HOOC)Ph                                                    1-637 4 NHCO -- 4-(HOOC)Ph                                                    1-638 4 NHCO -- 2-(MeOOC)Ph                                                   1-639 4 NHCO -- 4-(MeOOC)Ph                                                   1-640 4 NHCO -- 2-(EtOOC)Ph                                                   1-641 4 NHCO -- 4-(EtOOC)Ph                                                   1-642 4 NHCO -- 2-(tBuOOC)Ph                                                  1-643 4 NHCO -- 4-(tBuOOC)Ph                                                  1-644 4 NHCO -- 2-Cl--Ph                                                      1-645 4 NHCO -- 4-Cl--Ph                                                      1-646 4 NHCO -- 2-Br--Ph                                                      1-647 4 NHCO -- 4-Br--Ph                                                      1-648 4 NHCO -- 2-I--Ph                                                       1-649 4 NHCO -- 4-I--Ph                                                       1-650 4 NHCO -- 2-NO.sub.2 --Ph                                               1-651 4 NHCO -- 4-NO.sub.2 --Ph                                               1-652 4 NHCO -- 2-NH.sub.2 --Ph                                               1-653 4 NHCO -- 4-NH.sub.2 --Ph                                               1-654 4 NHCO -- 2-(HO.sub.3 S)Ph                                              1-655 4 NHCO -- 4-(HO.sub.3 S)Ph                                              1-656 4 NHCO -- 2-(NH.sub.2 O.sub.2 S)Ph                                      1-657 4 NHCO -- 4-(NH.sub.2 O.sub.2 S)Ph                                      1-658 4 NHCO -- 2-CN--Ph                                                      1-659 4 NHCO -- 4-CN--Ph                                                      1-660 4 NHCO -- 2-(HOCH.sub.2)Ph                                              1-661 4 NHCO -- 4-(HOCH.sub.2)Ph                                              1-662 4 NHCO -- Me                                                            1-663 4 NHCO -- Et                                                            1-664 4 NHCO -- Pr                                                            1-665 4 NHCO -- iPr                                                           1-666 4 NHCO -- Bu                                                            1-667 4 NHCO -- HOOCCH.sub.2 --                                               1-668 4 NHCO -- MeOOCCH.sub.2 --                                              1-669 4 NHCO -- MeCH(COOH)                                                    1-670 4 NHCO -- HOOC--(CH.sub.2).sub.2 --                                     1-671 4 NHCO -- MeCH(COOMe)                                                   1-672 4 NHCO -- 1-HOOC-iBu                                                    1-673 4 NHCO -- 1-HOOC-iPn                                                    1-674 4 NHCO -- 1-HOOC-2-Me--Bu                                               1-675 4 NHCO -- CH.sub.2 CH.sub.2 SO.sub.3 H                                  1-676 4 NHCO -- MeO                                                           1-677 4 NHCO -- EtO                                                           1-678 4 NHCO -- PrO                                                           1-679 4 NHCO -- Z-1                                                           1-680 4 NHCO -- Z-2                                                           1-681 4 NHCO -- Z-3                                                           1-682 4 NHCO -- Z-4                                                           1-683 4 NHCO -- Z-5                                                           1-684 4 NHCO -- Z-6                                                           1-685 4 NHCO -- Z-7                                                           1-686 4 NHCO -- Z-8                                                           1-687 4 NHCO -- Z-9                                                           1-688 4 NHCO -- Z-10                                                          1-689 4 NHCO -- Z-11                                                          1-690 4 NHCO -- Z-12                                                          1-691 4 NHCO -- 3-Py                                                          1-692 4 NHCO -- 4-Py                                                          1-693 4 NHCO NH H                                                             1-694 4 NHCO NH Ph                                                            1-695 4 NHCO NH 2-Me--Ph                                                      1-696 4 NHCO NH 4-Me--Ph                                                      1-697 4 NHCO NH 2,4-diMe--Ph                                                  1-698 4 NHCO NH 3,4-diMe--Ph                                                  1-699 4 NHCO NH 2-(CF.sub.3)Ph                                                1-700 4 NHCO NH 4-(CF.sub.3)Ph                                                1-701 4 NHCO NH 2-MeOPh                                                       1-702 4 NHCO NH 4-MeOPh                                                       1-703 4 NHCO NH 2-EtOPh                                                       1-704 4 NHCO NH 4-EtOPh                                                       1-705 4 NHCO NH 2-HOPh                                                        1-706 4 NHCO NH 4-HOPh                                                        1-707 4 NHCO NH 2-(HOOC)Ph                                                    1-708 4 NHCO NH 4-(HOOC)Ph                                                    1-709 4 NHCO NH 2-(MeOOC)Ph                                                   1-710 4 NHCO NH 4-(MeOOC)Ph                                                   1-711 4 NHCO NH 2-(EtOOC)Ph                                                   1-712 4 NHCO NH 4-(EtOOC)Ph                                                   1-713 4 NHCO NH 2-(tBuOOC)Ph                                                  1-714 4 NHCO NH 4-(tBuOOC)Ph                                                  1-715 4 NHCO NH 2-Cl--Ph                                                      1-716 4 NHCO NH 4-Cl--Ph                                                      1-717 4 NHCO NH 2-Br--Ph                                                      1-718 4 NHCO NH 4-Br--Ph                                                      1-719 4 NHCO NH 2-I--Ph                                                       1-720 4 NHCO NH 4-I--Ph                                                       1-721 4 NHCO NH 2-NO.sub.2 --Ph                                               1-722 4 NHCO NH 4-NO.sub.2 --Ph                                               1-723 4 NHCO NH 2-NH.sub.2 --Ph                                               1-724 4 NHCO NH 4-NH.sub.2 --Ph                                               1-725 4 NHCO NH 2-(HO.sub.3 S)Ph                                              1-726 4 NHCO NH 4-(HO.sub.3 S)Ph                                              1-727 4 NHCO NH 2-(NH.sub.2 O.sub.2 S)Ph                                      1-728 4 NHCO NH 4-(NH.sub.2 O.sub.2 S)Ph                                      1-729 4 NHCO NH 2-CN--Ph                                                      1-730 4 NHCO NH 4-CN--Ph                                                      1-731 4 NHCO NH 2-(HOCH.sub.2)Ph                                              1-732 4 NHCO NH 4-(HOCH.sub.2)Ph                                              1-733 4 NHCO NH Me                                                            1-734 4 NHCO NH Et                                                            1-735 4 NHCO NH Pr                                                            1-736 4 NHCO NH iPr                                                           1-737 4 NHCO NH Bu                                                            1-738 4 NHCO NH HOOCCH.sub.2 --                                               1-739 4 NHCO NH MeOOCCH.sub.2 --                                              1-740 4 NHCO NH MeCH(COOH)                                                    1-741 4 NHCO NH HOOC--(CH.sub.2).sub.2 --                                     1-742 4 NHCO NH MeCH(COOMe)                                                   1-743 4 NHCO NH 1-HOOC-iBu                                                    1-744 4 NHCO NH 1-MeOOC-iBu                                                   1-745 4 NHCO NH 1-HOOC-iPn                                                    1-746 4 NHCO NH 1-MeOOC-iPn                                                   1-747 4 NHCO NH 1-HOOC-2-Me--Bu                                               1-748 4 NHCO NH 1-MeOOC-2-Me--Bu                                              1-749 4 NHCO NH CH.sub.2 CH.sub.2 SO.sub.3 H                                  1-750 4 NHCO NH OH                                                            1-751 4 NHCO NH MeO                                                           1-752 4 NHCO NH EtO                                                           1-753 4 NHCO NH PrO                                                           1-754 4 NHCO NH iPrO                                                          1-755 4 NHCO NH BuO                                                           1-756 4 NHCO NH iBuO                                                          1-757 4 NHCO NH sBuO                                                          1-758 4 NHCO NH tBuO                                                          1-759 4 NHCO NH HxO                                                           1-760 4 NHCO NH PhO                                                           1-761 4 NHCO NH BzO                                                           1-762 4 NHCO NH Z-1                                                           1-763 4 NHCO NH Z-2                                                           1-764 4 NHCO NH Z-3                                                           1-765 4 NHCO NH Z-4                                                           1-766 4 NHCO NH Z-5                                                           1-767 4 NHCO NH Z-6                                                           1-768 4 NHCO NH Z-7                                                           1-769 4 NHCO NH Z-8                                                           1-770 4 NHCO NH Z-9                                                           1-771 4 NHCO NH Z-10                                                          1-772 4 NHCO NH Z-11                                                          1-773 4 NHCO NH Z-12                                                          1-774 4 NHCO NH 3-Py                                                          1-775 4 NHCO NH 4-Py                                                          1-776 4 NHCO NMe Ph                                                           1-777 4 NHCO NMe 2-Me--Ph                                                     1-778 4 NHCO NMe 4-Me--Ph                                                     1-779 4 NHCO NMe 2,4-diMe--Ph                                                 1-780 4 NHCO NMe 3,4-diMe--Ph                                                 1-781 4 NHCO NMe 2-(CF.sub.3)Ph                                               1-782 4 NHCO NMe 4-(CF.sub.3)Ph                                               1-783 4 NHCO NMe 2-MeOPh                                                      1-784 4 NHCO NMe 4-MeOPh                                                      1-785 4 NHCO NMe 2-EtOPh                                                      1-786 4 NHCO NMe 4-EtOPh                                                      1-787 4 NHCO NMe 2-HOPh                                                       1-788 4 NHCO NMe 4-HOPh                                                       1-789 4 NHCO NMe 2-(HOOC)Ph                                                   1-790 4 NHCO NMe 4-(HOOC)Ph                                                   1-791 4 NHCO NMe 2-(MeOOC)Ph                                                  1-792 4 NHCO NMe 4-(MeOOC)Ph                                                  1-793 4 NHCO NMe 2-(EtOOC)Ph                                                  1-794 4 NHCO NMe 4-(EtOOC)Ph                                                  1-795 4 NHCO NMe 2-(tBuOOC)Ph                                                 1-796 4 NHCO NMe 4-(tBuOOC)Ph                                                 1-797 4 NHCO NMe 2-Cl--Ph                                                     1-798 4 NHCO NMe 4-Cl--Ph                                                     1-799 4 NHCO NMe 2-Br--Ph                                                     1-800 4 NHCO NMe 4-Br--Ph                                                     1-801 4 NHCO NMe 2-I--Ph                                                      1-802 4 NHCO NMe 4-I--Ph                                                      1-803 4 NHCO NMe 2-NO.sub.2 --Ph                                              1-804 4 NHCO NMe 4-NO.sub.2 --Ph                                              1-805 4 NHCO NMe 2-NH.sub.2 --Ph                                              1-806 4 NHCO NMe 4-NH.sub.2 --Ph                                              1-807 4 NHCO NMe 2-(HO.sub.3 S)Ph                                             1-808 4 NHCO NMe 4-(HO.sub.3 S)Ph                                             1-809 4 NHCO NMe 2-(NH.sub.2 O.sub.2 S)Ph                                     1-810 4 NHCO NMe 4-(NH.sub.2 O.sub.2 S)Ph                                     1-811 4 NHCO NMe 2-CN--Ph                                                     1-812 4 NHCO NMe 4-CN--Ph                                                     1-813 4 NHCO NMe 2-(HOCH.sub.2)Ph                                             1-814 4 NHCO NMe 4-(HOCH.sub.2)Ph                                             1-815 4 NHCO NMe Me                                                           1-816 4 NHCO NMe Et                                                           1-817 4 NHCO NMe Pr                                                           1-818 4 NHCO NMe iPr                                                          1-819 4 NHCO NMe Bu                                                           1-820 4 NHCO NMe HOOCCH.sub.2 --                                              1-821 4 NHCO NMe MeOOCCH.sub.2 --                                             1-822 4 NHCO NMe MeCH(COOH)                                                   1-823 4 NHCO NMe HOOC--(CH.sub.2).sub.2 --                                    1-824 4 NHCO NMe MeCH(COOMe)                                                  1-825 4 NHCO NMe 1-HOOC-iBu                                                   1-826 4 NHCO NMe 1-MeOOC-iBu                                                  1-827 4 NHCO NMe 1-HOOC-iPn                                                   1-828 4 NHCO NMe 1-MeOOC-iPn                                                  1-829 4 NHCO NMe 1-HOOC-2-Me--Bu                                              1-830 4 NHCO NMe 1-MeOOC-2-Me--Bu                                             1-831 4 NHCO NMe CH.sub.2 CH.sub.2 SO.sub.3 H                                 1-832 4 NHCO NMe OH                                                           1-833 4 NHCO NMe MeO                                                          1-834 4 NHCO NMe EtO                                                          1-835 4 NHCO NMe PrO                                                          1-836 4 NHCO NMe iPrO                                                         1-837 4 NHCO NMe BuO                                                          1-838 4 NHCO NMe iBuO                                                         1-839 4 NHCO NMe sBuO                                                         1-840 4 NHCO NMe tBuO                                                         1-841 4 NHCO NMe HxO                                                          1-842 4 NHCO NMe PhO                                                          1-843 4 NHCO NMe BzO                                                          1-844 4 NHCO NMe Z-1                                                          1-845 4 NHCO NMe Z-2                                                          1-846 4 NHCO NMe Z-3                                                          1-847 4 NHCO NMe Z-4                                                          1-848 4 NHCO NMe Z-5                                                          1-849 4 NHCO NMe Z-6                                                          1-850 4 NHCO NMe Z-7                                                          1-851 4 NHCO NMe Z-8                                                          1-852 4 NHCO NMe Z-9                                                          1-853 4 NHCO NMe Z-10                                                         1-854 4 NHCO NMe Z-11                                                         1-855 4 NHCO NMe Z-12                                                         1-856 4 NHCO NMe 3-Py                                                         1-857 4 NHCO NMe 4-Py                                                         1-858 4 NHCO NHNH H                                                           1-859 4 NHCO NHNH Me                                                          1-860 4 NHCO NHNH Et                                                          1-861 4 NHCO NHNMe Me                                                         1-862 4 NHCO NHNMe Et                                                         1-863 4 NHCO NNNMe Pr                                                         1-864 4 NHCONHNHCO NH H                                                       1-865 4 NHCONHNHCO NH Ph                                                      1-866 4 NHCONHNHCO NH 2-Me--Ph                                                1-867 4 NHCONHNHCO NH 4-Me--Ph                                                1-868 4 NHCONHNHCO NH 2,4-diMe--Ph                                            1-869 4 NHCONHNHCO NH 3,4-diMe--Ph                                            1-870 4 NHCONHNHCO NH 2-(CF.sub.3)Ph                                          1-871 4 NHCONHNHCO NH 4-(CF.sub.3)Ph                                          1-872 4 NHCONHNHCO NH 2-MeOPh                                                 1-873 4 NHCONHNHCO NH 4-MeOPh                                                 1-874 4 NHCONHNHCO NH 2-EtOPh                                                 1-875 4 NHCONHNHCO NH 4-EtOPh                                                 1-876 4 NHCONHNHCO NH 2-HOPh                                                  1-877 4 NHCONHNHCO NH 4-HOPh                                                  1-878 4 NHCONHNHCO NH 2-(HOOC)Ph                                              1-879 4 NHCONHNHCO NH 4-(HOOC)Ph                                              1-880 4 NHCONMNHCO NH 2-(MeOOC)Ph                                             1-881 4 NHCONHNHCO NH 4-(MeOOC)Ph                                             1-882 4 NHCONHNHCO NH 2-(EtOOC)Ph                                             1-883 4 NHCONHNHCO NH 4-(EtOOC)Ph                                             1-884 4 NHCONHNHCO NH 2-(tBuOOC)Ph                                            1-885 4 NHCONHNHCO NH 4-(tBuOOC)Ph                                            1-886 4 NHCONHNHCO NH 2-Cl--Ph                                                1-887 4 NHCONHNHCO NH 4-Cl--Ph                                                1-888 4 NHCONHNHCO NH 2-Br--Ph                                                1-889 4 NHCONHNHCO NH 4-Br--Ph                                                1-890 4 NHCONHNHCO NH 2-I--Ph                                                 1-891 4 NHCONHNHCO NH 4-I--Ph                                                 1-892 4 NHCONHNHCO NH 2-NO.sub.2 --Ph                                         1-893 4 NHCONHNHCO NH 4-NO.sub.2 --Ph                                         1-894 4 NHCONHNHCO NH 2-NH.sub.2 --Ph                                         1-895 4 NHCONHNHCO NH 4-NH.sub.2 --Ph                                         1-896 4 NHCONHNHCO NH 2-(HO.sub.3 S)Ph                                        1-897 4 NHCONHNHCO NH 4-(HO.sub.3 S)Ph                                        1-898 4 NHCONHNHCO NH 2-(NH.sub.2 O.sub.2 S)Ph                                1-899 4 NHCONHNHCO NH 4-(NH.sub.2 O.sub.2 S)Ph                                1-900 4 NHCONHNHCO NH 2-CN--Ph                                                1-901 4 NHCONHNHCO NH 4-CN--Ph                                                1-902 4 NHCONHNHCO NH 2-(HOCH.sub.2)Ph                                        1-903 4 NHCONHNHCO NH 4-(HOCH.sub.2)Ph                                        1-904 4 NHCONHNHCO NH Me                                                      1-905 4 NHCONHNHCO NH Et                                                      1-906 4 NHCONHNHCO NH Pr                                                      1-907 4 NHCONHNHCO NH iPr                                                     1-908 4 NHCONHNHCO NH Bu                                                      1-909 4 NHCONHNHCO NH HOOCCH.sub.2 --                                         1-910 4 NHCONHNHCO NH MeOOCCH.sub.2 --                                        1-911 4 NHCONHNHCO NH MeCH(COOH)                                              1-912 4 NHCONHNHCO NH HOOC--(CH.sub.2).sub.2 --                               1-913 4 NHCONHNHCO NH MeCH(COOMe)                                             1-914 4 NHCONHNHCO NH 1-HOOC-iBu                                              1-915 4 NHCONHNHCO NH 1-MeOOC-iBu                                             1-916 4 NHCONHNHCO NH 1-HOOC-iPn                                              1-917 4 NHCONHNHCO NH 1-MeOOC-iPn                                             1-918 4 NHCONHNHCO NH 1-HOOC-2-Me--Bu                                         1-919 4 NHCONHNHCO NH 1-MeOOC-2-Me--Bu                                        1-920 4 NHCONHNHCO NH CH.sub.2 CH.sub.2 SO.sub.3 H                            1-921 4 NHCONHNHCO NH OH                                                      1-922 4 NHCONHNHCO NH MeO                                                     1-923 4 NHCONHNHCO NH EtO                                                     1-924 4 NHCONHNHCO NH PrO                                                     1-925 4 NHCONHNHCO NH iPrO                                                    1-926 4 NHCONHNHCO NH BuO                                                     1-927 4 NHCONHNHCO NH iBuO                                                    1-928 4 NHCONHNHCO NH sBuO                                                    1-929 4 NHCONHNHCO NH tBuO                                                    1-930 4 NHCONHNHCO NH HxO                                                     1-931 4 NHCONHNHCO NH PhO                                                     1-932 4 NHCONHNHCO NH BzO                                                     1-933 4 NHCONHNHCO NH Z-1                                                     1-934 4 NHCONHNHCO NH Z-2                                                     1-935 4 NHCONHNHCO NH Z-3                                                     1-936 4 NHCONHNHCO NH Z-4                                                     1-937 4 NHCONHNHCO NH Z-5                                                     1-938 4 NHCONHNHCO NH Z-6                                                     1-939 4 NHCONHNHCO NH Z-7                                                     1-940 4 NHCONHNHCO NH Z-8                                                     1-941 4 NHCONHNHCO NH Z-9                                                     1-942 4 NHCONHNHCO NH Z-10                                                    1-943 4 NHCONHNHCO NH Z-11                                                    1-944 4 NHCONHNHCO NH Z-12                                                    1-945 4 NHCONHNHCO NH 3-Py                                                    1-946 4 NHCONHNHCO NH 4-Py                                                    1-947 4 NHCONHCO -- H                                                         1-948 4 NHCONHCO -- Ph                                                        1-949 4 NHCONHCO -- 2-Me--Ph                                                  1-950 4 NHCONHCO -- 4-Me--Ph                                                  1-951 4 NHCONHCO -- 2,4-diMe--Ph                                              1-952 4 NHCONHCO -- 3,4-diMe--Ph                                              1-953 4 NHCONHCO -- 2-(CF.sub.3)Ph                                            1-954 4 NHCONHCO -- 4-(CF.sub.3)Ph                                            1-955 4 NHCONHCO -- 2-MeOPh                                                   1-956 4 NHCONHCO -- 4-MeOPh                                                   1-957 4 NHCONHCO -- 2-EtOPh                                                   1-958 4 NHCONHCO -- 4-EtOPh                                                   1-959 4 NHCONHCO -- 2-HOPh                                                    1-960 4 NHCONHCO -- 4-HOPh                                                    1-961 4 NHCONHCO -- 2-(HOOC)Ph                                                1-962 4 NHCONHCO -- 4-(HOOC)Ph                                                1-963 4 NHCONHCO -- 2-(MeOOC)Ph                                               1-964 4 NHCONHCO -- 4-(MeOOC)Ph                                               1-965 4 NHCONHCO -- 2-(EtOOC)Ph                                               1-966 4 NHCONHCO -- 4-(EtOOC)Ph                                               1-967 4 NHCONHCO -- 2-(tBuOOC)Ph                                              1-968 4 NHCONHCO -- 4-(tBuOOC)Ph                                              1-969 4 NHCONHCO -- 2-Cl--Ph                                                  1-970 4 NHCONHCO -- 4-Cl--Ph                                                  1-971 4 NHCONHCO -- 2-Br--Ph                                                  1-972 4 NHCONHCO -- 4-Br--Ph                                                  1-973 4 NHCONHCO -- 2-I--Ph                                                   1-974 4 NHCONHCO -- 4-I--Ph                                                   1-975 4 NHCONHCO -- 2-NO.sub.2 --Ph                                           1-976 4 NHCONHCO -- 4-NO.sub.2 --Ph                                           1-977 4 NHCONHCO -- 2-NH.sub.2 --Ph                                           1-978 4 NHCONHCO -- 4-NH.sub.2 --Ph                                           1-979 4 NHCONHCO -- 2-(HO.sub.3 S)Ph                                          1-980 4 NHCONHCO -- 4-(HO.sub.3 S)Ph                                          1-981 4 NHCONHCO -- 2-(NH.sub.2 O.sub.2 S)Ph                                  1-982 4 NHCONHCO -- 4-(NH.sub.2 O.sub.2 S)Ph                                  1-983 4 NHCONHCO -- 2-CN--Ph                                                  1-984 4 NHCONHCO -- 4-CN--Ph                                                  1-985 4 NHCONHCO -- 2-(HOCH.sub.2)Ph                                          1-986 4 NHCONHCO -- 4-(HOCH.sub.2)Ph                                          1-987 4 NHCONHCO -- Me                                                        1-988 4 NHCONHCO -- Et                                                        1-989 4 NHCONHCO -- Pr                                                        1-990 4 NHCONHCO -- iPr                                                       1-991 4 NHCONHCO -- Bu                                                        1-992 4 NHCONHCO -- HOOCCH.sub.2 --                                           1-993 4 NHCONHCO -- MeOOCCH.sub.2 --                                          1-994 4 NHCONHCO -- MeCH(COOH)                                                1-995 4 NHCONHCO -- HOOC--(CH.sub.2).sub.2 --                                 1-996 4 NHCONHCO -- MeCH(COOMe)                                               1-997 4 NHCONHCO -- 1-HOOC-iBu                                                1-998 4 NHCONHCO -- 1-MeOOC-iBu                                               1-999 4 NHCONHCO -- 1-HOOC-iPn                                                1-1000 4 NHCONHCO -- 1-MeOOC-iPn                                              1-1001 4 NHCONHCO -- 1-HOOC-2-Me--Bu                                          1-1002 4 NHCONHCO -- 1-MeOOC-2-Me--Bu                                         1-1003 4 NHCONHCO -- CH.sub.2 CH.sub.2 SO.sub.3 H                             1-1004 4 NHCONHCO -- MeO                                                      1-1005 4 NHCONHCO -- EtO                                                      1-1006 4 NHCONHCO -- PrO                                                      1-1007 4 NHCONHCO -- iPrO                                                     1-1008 4 NHCONHCO -- BuO                                                      1-1009 4 NHCONHCO -- iBuO                                                     1-1010 4 NHCONHCO -- sBuO                                                     1-1011 4 NHCONHCO -- tBuO                                                     1-1012 4 NHCONHCO -- HxO                                                      1-1013 4 NHCONHCO -- PhO                                                      1-1014 4 NHCONHCO -- BzO                                                      1-1015 4 NHCONHCO -- Z-1                                                      1-1016 4 NHCONHCO -- Z-2                                                      1-1017 4 NHCONHCO -- Z-3                                                      1-1018 4 NHCONHCO -- Z-4                                                      1-1019 4 NHCONHCO -- Z-5                                                      1-1020 4 NHCONHCO -- Z-6                                                      1-1021 4 NHCONHCO -- Z-7                                                      1-1022 4 NHCONHCO -- Z-8                                                      1-1023 4 NHCONHCO -- Z-9                                                      1-1024 4 NHCONHCO -- Z-10                                                     1-1025 4 NHCONHCO -- Z-11                                                     1-1026 4 NHCONHCO -- Z-12                                                     1-1027 4 NHCONHCO -- 3-Py                                                     1-1028 4 NHCONHCO -- 4-Py                                                     1-1029 4 NHCONHSO.sub.2 -- H                                                  1-1030 4 NHCONHSO.sub.2 -- Ph                                                 1-1031 4 NHCONHSO.sub.2 -- 2-Me--Ph                                           1-1032 4 NHCONHSO.sub.2 -- 4-Me--Ph                                           1-1033 4 NHCONHSO.sub.2 -- 2,4-diMe--Ph                                       1-1034 4 NHCONHSO.sub.2 -- 3,4-diMe--Ph                                       1-1035 4 NHCONHSO.sub.2 -- 2-(CF.sub.3)Ph                                     1-1036 4 NHCONHSO.sub.2 -- 4-(CF.sub.3)Ph                                     1-1037 4 NHCONHSO.sub.2 -- 2-MeOPh                                            1-1038 4 NHCONHSO.sub.2 -- 4-MeOPh                                            1-1039 4 NHCONHSO.sub.2 -- 2-EtOPh                                            1-1040 4 NHCONHSO.sub.2 -- 4-EtOPh                                            1-1041 4 NHCONHSO.sub.2 -- 2-HOPh                                             1-1042 4 NHCONHSO.sub.2 -- 4-HOPh                                             1-1043 4 NHCONHSO.sub.2 -- 2-(HOOC)Ph                                         1-1044 4 NHCONHSO.sub.2 -- 4-(HOOC)Ph                                         1-1045 4 NHCONHSO.sub.2 -- 2-(MeOOC)Ph                                        1-1046 4 NHCONHSO.sub.2 -- 4-(MeOOC)Ph                                        1-1047 4 NHCONHSO.sub.2 -- 2-(EtOOC)Ph                                        1-1048 4 NHCONHSO.sub.2 -- 4-(EtOOC)Ph                                        1-1049 4 NHCONHSO.sub.2 -- 2-(tBuOOC)Ph                                       1-1050 4 NHCONHSO.sub.2 -- 4-(tBuOOC)Ph                                       1-1051 4 NHCONHSO.sub.2 -- 2-Cl--Ph                                           1-1052 4 NHCONHSO.sub.2 -- 4-Cl--Ph                                           1-1053 4 NHCONHSO.sub.2 -- 2-Br--Ph                                           1-1054 4 NHCONHSO.sub.2 -- 4-Br--Ph                                           1-1055 4 NHCONHSO.sub.2 -- 2-I--Ph                                            1-1056 4 NHCONHSO.sub.2 -- 4-I--Ph                                            1-1057 4 NHCONHSO.sub.2 -- 2-NO.sub.2 --Ph                                    1-1058 4 NHCONHSO.sub.2 -- 4-NO.sub.2 --Ph                                    1-1059 4 NHCONHSO.sub.2 -- 2-NH.sub.2 --Ph                                    1-1060 4 NHCONHSO.sub.2 -- 4-NH.sub.2 --Ph                                    1-1061 4 NHCONHSO.sub.2 -- 2-(HO.sub.3 S)Ph                                   1-1062 4 NHCONHSO.sub.2 -- 4-(HO.sub.3 S)Ph                                   1-1063 4 NHCONHSO.sub.2 -- 2-(NH.sub.2 O.sub.2 S)Ph                           1-1064 4 NHCONHSO.sub.2 -- 4-(NH.sub.2 O.sub.2 S)Ph                           1-1065 4 NHCONHSO.sub.2 -- 2-CN--Ph                                           1-1066 4 NHCONHSO.sub.2 -- 4-CN--Ph                                           1-1067 4 NHCONHSO.sub.2 -- 2-(HOCH.sub.2)Ph                                   1-1068 4 NHCONHSO.sub.2 -- 4-(HOCH.sub.2)Ph                                   1-1069 4 NHCONHSO.sub.2 -- Me                                                 1-1070 4 NHCONHSO.sub.2 -- Et                                                 1-1071 4 NHCONHSO.sub.2 -- Pr                                                 1-1072 4 NHCONHSO.sub.2 -- iPr                                                1-1073 4 NHCONHSO.sub.2 -- Bu                                                 1-1074 4 NHCONHSO.sub.2 -- HOOCCH.sub.2 --                                    1-1075 4 NHCONHSO.sub.2 -- MeOOCCH.sub.2 --                                   1-1076 4 NHCONHSO.sub.2 -- MeCH(COOH)                                         1-1077 4 NHCONHSO.sub.2 -- HOOC--(CH.sub.2).sub.2 --                          1-1078 4 NHCONHSO.sub.2 -- MeCH(COOMe)                                        1-1079 4 NHCONHSO.sub.2 -- 1-HOOC-iBu                                         1-1080 4 NHCONHSO.sub.2 -- 1-MeOOC-iBu                                        1-1081 4 NHCONHSO.sub.2 -- 1-HOOC-iPn                                         1-1082 4 NHCONHSO.sub.2 -- 1-MeOOC-iPn                                        1-1083 4 NHCONHSO.sub.2 -- 1-HOOC-2-Me--Bu                                    1-1084 4 NHCONHSO.sub.2 -- 1-MeOOC-2-Me--Bu                                   1-1085 4 NHCONHSO.sub.2 -- CH.sub.2 CH.sub.2 SO.sub.3 H                       1-1086 4 NHCONHSO.sub.2 -- OH                                                 1-1087 4 NHCONHSO.sub.2 -- MeO                                                1-1088 4 NHCONHSO.sub.2 -- EtO                                                1-1089 4 NHCONHSO.sub.2 -- PrO                                                1-1090 4 NHCONHSO.sub.2 -- iPrO                                               1-1091 4 NHCONHSO.sub.2 -- BuO                                                1-1092 4 NHCONHSO.sub.2 -- iBuO                                               1-1093 4 NHCONHSO.sub.2 -- sBuO                                               1-1094 4 NHCONHSO.sub.2 -- tBuO                                               1-1095 4 NHCONHSO.sub.2 -- HxO                                                1-1096 4 NHCONHSO.sub.2 -- PhO                                                1-1097 4 NHCONHSO.sub.2 -- BzO                                                1-1098 4 NHCONHSO.sub.2 -- Z-1                                                1-1099 4 NHCONHSO.sub.2 -- Z-2                                                1-1100 4 NHCONHSO.sub.2 -- Z-3                                                1-1101 4 NHCONHSO.sub.2 -- Z-4                                                1-1102 4 NHCONHSO.sub.2 -- Z-5                                                1-1103 4 NHCONHSO.sub.2 -- Z-6                                                1-1104 4 NHCONHSO.sub.2 -- Z-7                                                1-1105 4 NHCONHSO.sub.2 -- Z-8                                                1-1106 4 NHCONHSO.sub.2 -- Z-9                                                1-1107 4 NHCONHSO.sub.2 -- Z-10                                               1-1108 4 NHCONHSO.sub.2 -- Z-11                                               1-1109 4 NHCONHSO.sub.2 -- Z-12                                               1-1110 4 NHCONHSO.sub.2 -- 3-Py                                               1-1111 4 NHCONHSO.sub.2 -- 4-Py                                               1-1112 4 NHCONHSO.sub.2 NH H                                                  1-1113 4 NHCONHSO.sub.2 NH Me                                                 1-1114 4 NHCONHSO.sub.2 NH Et                                                 1-1115 4 NHCONHSO.sub.2 NH Pr                                                 1-1116 4 NHCONHSO.sub.2 NH iPr                                                1-1117 4 NHCONHSO.sub.2 NH Bu                                                 1-1118 4 NHCONHSO.sub.2 NMe Me                                                1-1119 4 NHCONHSO.sub.2 NMe Et                                                1-1120 4 NHCONHSO.sub.2 NMe Pr                                                1-1121 4 NHCONHSO.sub.2 NMe iPr                                               1-1122 4 NHCONHSO.sub.2 NMe Bu                                                1-1123 4 -- NH H                                                              1-1124 4 -- NH Me                                                             1-1125 4 -- NH Et                                                             1-1126 4 -- NH Pr                                                             1-1127 4 -- NH iPr                                                            1-1128 4 -- NH Bu                                                           1-1129                                                                            4   CO         Pyr                                                          1-1130 4 CO Pipri                                                             1-1131 4 CO Pipra                                                             1-1132 4 CO Mor                                                               1-1133 4 CO Thmor                                                             1-1134 4 CO NHPyr                                                             1-1135 4 CO NHPipri                                                           1-1136 4 CO NHPipra                                                           1-1137 4 CO NHMor                                                             1-1138 4 CO NHThmor                                                           1-1139 4 NHCO Pyr                                                             1-1140 4 NHCO Pipri                                                           1-1141 4 NHCO Pipra                                                           1-1142 4 NHCO Mor                                                             1-1143 4 NHCO Thmor                                                           1-1144 4 NHCO NHPyr                                                           1-1145 4 NHCO NHPipri                                                         1-1146 4 NHCO NHPipra                                                         1-1147 4 NHCO NHMor                                                           1-1148 4 NHCO NHThmor                                                         1-1149 4 CONHCO Pyr                                                           1-1150 4 CONHCO Pipri                                                         1-1151 4 CONHCO Pipra                                                         1-1152 4 CONHCO Mor                                                           1-1153 4 CONHCO Thmor                                                         1-1154 4 CONHCO NHPyr                                                         1-1155 4 CONHCO NHPipri                                                       1-1156 4 CONHCO NHPipra                                                       1-1157 4 CONHCO NHMor                                                         1-1158 4 CONHCO NHThmor                                                       1-1159 4 CONHSO.sub.2 Pyr                                                     1-1160 4 CONHSO.sub.2 Pipri                                                   1-1161 4 CONHSO.sub.2 Pipra                                                   1-1162 4 CONHSO.sub.2 Mor                                                     1-1163 4 CONHSO.sub.2 Thmor                                                   1-1164 4 CONHSO.sub.2 NHPyr                                                   1-1165 4 CONHSO.sub.2 NHPipri                                                 1-1166 4 CONHSO.sub.2 NHPipra                                                 1-1167 4 CONHSO.sub.2 NHMor                                                   1-1168 4 CONHSO.sub.2 NHThmor                                               1-1169                                                                            4   NHSO.sub.2 NH     Z-4                                                   1-1170 4 NHSO.sub.2 -- Me                                                     1-1171 4 NHSO.sub.2 -- Et                                                     1-1172 4 NHSO.sub.2 -- Pr                                                     1-1173 4 NHSO.sub.2 -- CH.sub.2 Cl                                            1-1174 4 NHSO.sub.2 -- Ph                                                     1-1175 4 NHSO.sub.2 -- 4-Me--Ph                                               1-1176 4 CO NMe Ph                                                            1-1177 4 CO NMe 2-Me--Ph                                                      1-1178 4 CO NMe 4-Me--Ph                                                      1-1179 4 CO NMe 2,4-diMe--Ph                                                  1-1180 4 CO NMe 3,4-diMe--Ph                                                  1-1181 4 CO NMe 2-(CF.sub.3)Ph                                                1-1182 4 CO NMe 4-(CF.sub.3)Ph                                                1-1183 4 CO NMe 2-MeOPh                                                       1-1184 4 CO NMe 4-MeOPh                                                       1-1185 4 CO NMe 2-EtOPh                                                       1-1186 4 CO NMe 4-EtOPh                                                       1-1187 4 CO NMe 2-HOPh                                                        1-1188 4 CO NMe 4-HOPh                                                        1-1189 4 CO NMe 2-(HOOC)Ph                                                    1-1190 4 CO NMe 4-(HOOC)Ph                                                    1-1191 4 CO NMe 2-(MeOOC)Ph                                                   1-1192 4 CO NMe 4-(MeOOC)Ph                                                   1-1193 4 CO NMe 2-(EtOOC)Ph                                                   1-1194 4 CO NMe 4-(EtOOC)Ph                                                   1-1195 4 CO NMe 2-(tBuOOC)Ph                                                  1-1196 4 CO NMe 4-(tBuOOC)Ph                                                  1-1197 4 CO NMe 2-Cl--Ph                                                      1-1198 4 CO NMe 4-Cl--Ph                                                      1-1199 4 CO NMe 2-Br--Ph                                                      1-1200 4 CO NMe 4-Br--Ph                                                      1-1201 4 CO NMe 2-I--Ph                                                       1-1202 4 CO NMe 4-I--Ph                                                       1-1203 4 CO NMe 2-NO.sub.2 --Ph                                               1-1204 4 CO NMe 4-NO.sub.2 --Ph                                               1-1205 4 CO NMe 2-NH.sub.2 --Ph                                               1-1206 4 CO NMe 4-NH.sub.2 --Ph                                               1-1207 4 CO NMe 2-(HO.sub.3 S)Ph                                              1-1208 4 CO NMe 4-(HO.sub.3 S)Ph                                              1-1209 4 CO NMe 2-(NH.sub.2 O.sub.2 S)Ph                                      1-1210 4 CO NMe 4-(NH.sub.2 O.sub.2 S)Ph                                      1-1211 4 CO NMe 2-CN--Ph                                                      1-1212 4 CO NMe 4-CN--Ph                                                      1-1213 4 CO NMe 2-(HOCH.sub.2)Ph                                              1-1214 4 CO NMe 4-(HOCH.sub.2)Ph                                              1-1215 4 CO NMe Me                                                            1-1216 4 CO NMe Et                                                            1-1217 4 CO NMe Pr                                                            1-1218 4 CO NMe iPr                                                           1-1219 4 CO NMe Bu                                                            1-1220 4 CO NMe HOOCCH.sub.2 --                                               1-1221 4 CO NMe MeOOCCH.sub.2 --                                              1-1222 4 CO NMe MeCH(COOH)                                                    1-1223 4 CO NMe HOOC--(CH.sub.2).sub.2 --                                     1-1224 4 CO NMe MeCH(COOMe)                                                   1-1225 4 CO NMe 1-HOOC-iBu                                                    1-1226 4 CO NMe 1-MeOOC-iBu                                                   1-1227 4 CO NMe 1-HOOC-iPn                                                    1-1228 4 CO NMe 1-MeOOC-iPn                                                   1-1229 4 CO NMe 1-HOOC-2-Me--Bu                                               1-1230 4 CO NMe 1-MeOOC-2-Me--Bu                                              1-1231 4 CO NMe CH.sub.2 CH.sub.2 SO.sub.3 H                                  1-1232 4 CO NMe OH                                                            1-1233 4 CO NMe MeO                                                           1-1234 4 CO NMe EtO                                                           1-1235 4 CO NMe PrO                                                           1-1236 4 CO NMe iPrO                                                          1-1237 4 CO NMe BuO                                                           1-1238 4 CO NMe iBuO                                                          1-1239 4 CO NMe sBuO                                                          1-1240 4 CO NMe tBuO                                                          1-1241 4 CO NMe HxO                                                           1-1242 4 CO NMe PhO                                                           1-1243 4 CO NMe BzO                                                           1-1244 4 CO NMe Z-1                                                           1-1245 4 CO NMe Z-2                                                           1-1246 4 CO NMe Z-3                                                           1-1247 4 CO NMe Z-4                                                           1-1248 4 CO NMe Z-5                                                           1-1249 4 CO NMe Z-6                                                           1-1250 4 CO NMe Z-7                                                           1-1251 4 CO NMe Z-8                                                           1-1252 4 CO NMe Z-9                                                           1-1253 4 CO NMe Z-10                                                          1-1254 4 CO NMe Z-11                                                          1-1255 4 CO NMe Z-12                                                          1-1256 4 CO NMe 3-Py                                                          1-1257 4 CO NMe 4-Py                                                        1-1258                                                                            4  CO          Thiad                                                        1-1259 4 CO NHThiad                                                           1-1260 4 NHCO Thiad                                                           1-1261 4 NHCO NHThiad                                                         1-1262 4 CONHCO Thiad                                                         1-1263 4 CONHCO NHThiad                                                       1-1264 4 CONHSO.sub.2 Thiad                                                   1-1265 4 CONHSO.sub.2 NHThiad                                               1-1266                                                                            4   NHCS       NH     H                                                     1-1267 4 NHCS NH Me                                                           1-1268 4 NHCS NH Et                                                           1-1269 4 NHCS NH Ph                                                           1-1270 4 NHCS NH HOOCCH.sub.2 --                                              1-1271 4 NHCS NH MeOOCCH.sub.2 --                                             1-1272 4 NHCS NH MeCH(COOH)                                                   1-1273 4 NHCS NH HOOC--(CH.sub.2).sub.2 --                                    1-1274 4 NHCS NH MeCH(COOMe)                                                  1-1275 4 CO NH HOOC--(CH.sub.2).sub.3 --                                      1-1276 4 NHCO NH HOOC--(CH.sub.2).sub.3 --                                    1-1277 4 NHCO -- HOOC--(CH.sub.2).sub.3 --                                    1-1278 4 NHCS NH HOOC--(CH.sub.2).sub.3 --                                    1-1279 4 CO NH MeSO.sub.2 NHCOCH(Me)                                          1-1280 4 NHCO NH MeSO.sub.2 NHCOCH(Me)                                        1-1281 4 NHCO -- MeSO.sub.2 NHCOCH(Me)                                        1-1282 4 NHCS NH MeSO.sub.2 NHCOCH(Me)                                        1-1283 4 -- NH HOOCCH.sub.2 --                                                1-1284 4 -- NH MeOOCCH.sub.2 --                                               1-1285 4 -- NH MeCH(COOH)                                                     1-1286 4 -- NH HOOC--(CH.sub.2).sub.2 --                                      1-1287 4 -- NH MeCH(COOMe)                                                    1-1288 4 -- NH HOOC--(CH.sub.2).sub.3 --                                      1-1289 4 NHCOCO -- OH                                                         1-1290 4 NHCOCO -- MeO                                                        1-1291 4 NHCOCO -- EtO                                                        1-1292 4 NHCOCO -- PrO                                                        1-1293 4 NHCOCO -- iPrO                                                       1-1294 4 NHCOCO -- BuO                                                        1-1295 4 NHCOCO -- iBuO                                                       1-1296 4 NHCOCO -- sBuO                                                       1-1297 4 NHCOCO -- tBuO                                                       1-1298 4 NHCOCO -- HxO                                                        1-1299 4 NHCOCO -- PhO                                                        1-1300 4 NHCOCO -- BzO                                                        1-1301 5 CO NH H                                                              1-1302 5 CO NH Ph                                                             1-1303 5 CO NH 2-Me--Ph                                                       1-1304 5 CO NH 4-Me--Ph                                                       1-1305 5 CO NH 2,4-diMe--Ph                                                   1-1306 5 CO NH 3,4-diMe--Ph                                                   1-1307 5 CO NH 2-(CF.sub.3)Ph                                                 1-1308 5 CO NH 4-(CF.sub.3)Ph                                                 1-1309 5 CO NH 2-MeOPh                                                        1-1310 5 CO NH 4-MeOPh                                                        1-1311 5 CO NH 2-EtOPh                                                        1-1312 5 CO NH 4-EtOPh                                                        1-1313 5 CO NH 2-HOPh                                                         1-1314 5 CO NH 4-HOPh                                                         1-1315 5 CO NH 2-(HOOC)Ph                                                     1-1316 5 CO NH 4-(HOOC)Ph                                                     1-1317 5 CO NH 2-(MeOOC)Ph                                                    1-1318 5 CO NH 4-(MeOOC)Ph                                                    1-1319 5 CO NH 2-(EtOOC)Ph                                                    1-1320 5 CO NH 4-(EtOOC)Ph                                                    1-1321 5 CO NH 2-(tBuOOC)Ph                                                   1-1322 5 CO NH 4-(tBuOOC)Ph                                                   1-1323 5 CO NH 2-Cl--Ph                                                       1-1324 5 CO NH 4-Cl--Ph                                                       1-1325 5 CO NH 2-Br--Ph                                                       1-1326 5 CO NH 4-Br--Ph                                                       1-1327 5 CO NH 2-I--Ph                                                        1-1328 5 CO NH 4-I--Ph                                                        1-1329 5 CO NH 2-NO.sub.2 --Ph                                                1-1330 5 CO NH 4-NO.sub.2 --Ph                                                1-1331 5 CO NH 2-NH.sub.2 --Ph                                                1-1332 5 CO NH 4-NH.sub.2 --Ph                                                1-1333 5 CO NH 2-(HO.sub.3 S)Ph                                               1-1334 5 CO NH 4-(HO.sub.3 S)Ph                                               1-1335 5 CO NH 2-(NH.sub.2 O.sub.2 S)Ph                                       1-1336 5 CO NH 4-(NH.sub.2 O.sub.2 S)Ph                                       1-1337 5 CO NH 2-CN--Ph                                                       1-1338 5 CO NH 4-CN--Ph                                                       1-1339 5 CO NH 2-(HOCH.sub.2)Ph                                               1-1340 5 CO NH 4-(HOCH.sub.2)Ph                                               1-1341 5 CO NH Me                                                             1-1342 5 CO NH Et                                                             1-1343 5 CO NH Pr                                                             1-1344 5 CO NH iPr                                                            1-1345 5 CO NH Bu                                                             1-1346 5 CO NH HOOCCH.sub.2 --                                                1-1347 5 CO NH MeOOCCH.sub.2 --                                               1-1348 5 CO NH MeCH(COOH)                                                     1-1349 5 CO NH HOOC--(CH.sub.2).sub.2 --                                      1-1350 5 CO NH MeCH(COOMe)                                                    1-1351 5 CO NH 1-HOOC-iBu                                                     1-1352 5 CO NH 1-MeOOC-iBu                                                    1-1353 5 CO NH 1-HOOC-iPn                                                     1-1354 5 CO NH 1-MeOOC-iPn                                                    1-1355 5 CO NH 1-HOOC-2-Me--Bu                                                1-1356 5 CO NH 1-MeOOC-2-Me--Bu                                               1-1357 5 CO NH CH.sub.2 CH.sub.2 SO.sub.3 H                                   1-1358 5 CO NH OH                                                             1-1359 5 CO NH MeO                                                            1-1360 5 CO NH EtO                                                            1-1361 5 CO NH PrO                                                            1-1362 5 CO NH iPrO                                                           1-1363 5 CO NH BuO                                                            1-1364 5 CO NH iBuO                                                           1-1365 5 CO NH sBuO                                                           1-1366 5 CO NH tBuO                                                           1-1367 5 CO NH HxO                                                            1-1368 5 CO NH PhO                                                            1-1369 5 CO NH BzO                                                            1-1370 5 CO NH Z-1                                                            1-1371 5 CO NH Z-2                                                            1-1372 5 CO NH Z-3                                                            1-1373 5 CO NH Z-4                                                            1-1374 5 CO NH Z-5                                                            1-1375 5 CO NH Z-6                                                            1-1376 5 CO NH Z-7                                                            1-1377 5 CO NH Z-8                                                            1-1378 5 CO NH Z-9                                                            1-1379 5 CO NH Z-10                                                           1-1380 5 CO NH Z-11                                                           1-1381 5 CO NH Z-12                                                           1-1382 5 CO NH 3-Py                                                           1-1383 5 CO NH 4-Py                                                           1-1384 5 CO N(Ac) H                                                           1-1385 5 CO N(Ac) Ph                                                          1-1386 5 CO N(Ac) 2-Me--Ph                                                    1-1387 5 CO N(Ac) 4-Me--Ph                                                    1-1388 5 CO N(Ac) 2,4-diMe--Ph                                                1-1389 5 CO N(Ac) 3,4-diMe--Ph                                                1-1390 5 CO N(Ac) 2-(CF.sub.3)Ph                                              1-1391 5 CO N(Ac) 4-(CF.sub.3)Ph                                              1-1392 5 CO N(Ac) 2-MeOPh                                                     1-1393 5 CO N(Ac) 4-MeOPh                                                     1-1394 5 CO N(Ac) 2-EtOPh                                                     1-1395 5 CO N(Ac) 4-EtOPh                                                     1-1396 5 CO N(Ac) 2-HOPh                                                      1-1397 5 CO N(Ac) 4-HOPh                                                      1-1398 5 CO N(Ac) 2-(HOOC)Ph                                                  1-1399 5 CO N(Ac) 4-(HOOC)Ph                                                  1-1400 5 CO N(Ac) 2-(MeOOC)Ph                                                 1-1401 5 CO N(Ac) 4-(MeOOC)Ph                                                 1-1402 5 CO N(Ac) 2-(EtOOC)Ph                                                 1-1403 5 CO N(Ac) 4-(EtOOC)Ph                                                 1-1404 5 CO N(Ac) 2-(tBuOOC)Ph                                                1-1405 5 CO N(Ac) 4-(tBuOOC)Ph                                                1-1406 5 CO N(Ac) 2-Cl--Ph                                                    1-1407 5 CO N(Ac) 4-Cl--Ph                                                    1-1408 5 CO N(Ac) 2-Br--Ph                                                    1-1409 5 CO N(Ac) 4-Br--Ph                                                    1-1410 5 CO N(Ac) 2-I--Ph                                                     1-1411 5 CO N(Ac) 4-I--Ph                                                     1-1412 5 CO N(Ac) 2-NO.sub.2 --Ph                                             1-1413 5 CO N(Ac) 4-NO.sub.2 --Ph                                             1-1414 5 CO N(Ac) 2-NH.sub.2 --Ph                                             1-1415 5 CO N(Ac) 4-NH.sub.2 --Ph                                             1-1416 5 CO N(Ac) 2-(HO.sub.3 S)Ph                                            1-1417 5 CO N(Ac) 4-(HO.sub.3 S)Ph                                            1-1418 5 CO N(Ac) 2-(NH.sub.2 O.sub.2 S)Ph                                    1-1419 5 CO N(Ac) 4-(NH.sub.2 O.sub.2 S)Ph                                    1-1420 5 CO N(Ac) 2-CN--Ph                                                    1-1421 5 CO N(Ac) 4-CN--Ph                                                    1-1422 5 CO N(Ac) 2-(HOCH.sub.2)Ph                                            1-1423 5 CO N(Ac) 4-(HOCH.sub.2)Ph                                            1-1424 5 CO N(Ac) Me                                                          1-1425 5 CO N(Ac) Et                                                          1-1426 5 CO N(Ac) Pr                                                          1-1427 5 CO N(Ac) iPr                                                         1-1428 5 CO N(Ac) Bu                                                          1-1429 5 CO N(Ac) HOOCCH.sub.2 --                                             1-1430 5 CO N(Ac) MeOOCCH.sub.2 --                                            1-1431 5 CO N(Ac) MeCH(COOH)                                                  1-1432 5 CO N(Ac) HOOC--(CH.sub.2).sub.2 --                                   1-1433 5 CO N(Ac) MeCH(COOMe)                                                 1-1434 5 CO N(Ac) 1-HOOC-iBu                                                  1-1435 5 CO N(Ac) 1-MeOOC-iBu                                                 1-1436 5 CO N(Ac) 1-HOOC-iPn                                                  1-1437 5 CO N(Ac) 1-MeOOC-iPn                                                 1-1438 5 CO N(Ac) 1-HOOC-2-Me--Bu                                             1-1439 5 CO N(Ac) 1-MeOOC-2-Me--Bu                                            1-1440 5 CO N(Ac) CH.sub.2 CH.sub.2 SO.sub.3 H                                1-1441 5 CO N(Ac) OH                                                          1-1442 5 CO N(Ac) MeO                                                         1-1443 5 CO N(Ac) EtO                                                         1-1444 5 CO N(Ac) PrO                                                         1-4445 5 CO N(Ac) iPrO                                                        1-1446 5 CO N(Ac) BuO                                                         1-1447 5 CO N(Ac) iBuO                                                        1-1448 5 CO N(Ac) sBuO                                                        1-1449 5 CO N(Ac) tBuO                                                        1-1450 5 CO N(Ac) HxO                                                         1-1451 5 CO N(Ac) PhO                                                         1-1452 5 CO N(Ac) BzO                                                         1-1453 5 CO N(Ac) Z-1                                                         1-1454 5 CO N(Ac) Z-2                                                         1-1455 5 CO N(Ac) Z-3                                                         1-1456 5 CO N(Ac) Z-4                                                         1-1457 5 CO N(Ac) Z-5                                                         1-1458 5 CO N(Ac) Z-6                                                         1-1459 5 CO N(Ac) Z-7                                                         1-1460 5 CO N(Ac) Z-8                                                         1-1461 5 CO N(Ac) Z-9                                                         1-1462 5 CO N(Ac) Z-10                                                        1-1463 5 CO N(Ac) Z-11                                                        1-1464 5 CO N(Ac) Z-12                                                        1-1465 5 CO N(Ac) 3-Py                                                        1-1466 5 CO N(Ac) 4-Py                                                        1-1467 5 COO -- H                                                             1-1468 5 COO -- Ph                                                            1-1469 5 COO -- 2-Me--Ph                                                      1-1470 5 COO -- 4-Me--Ph                                                      1-1471 5 COO -- 2,4-diMe--Ph                                                  1-1472 5 COO -- 3,4-diMe--Ph                                                  1-1473 5 COO -- 2-(CF.sub.3)Ph                                                1-1474 5 COO -- 4-(CF.sub.3)Ph                                                1-1475 5 COO -- 2-MeOPh                                                       1-1476 5 COO -- 4-MeOPh                                                       1-1477 5 COO -- 2-EtOPh                                                       1-1478 5 COO -- 4-EtOPh                                                       1-1479 5 COO -- 2-HOPh                                                        1-1480 5 COO -- 4-HOPh                                                        1-1481 5 COO -- 2-(HOOC)Ph                                                    1-1482 5 COO -- 4-(HOOC)Ph                                                    1-1483 5 COO -- 2-(MeOOC)Ph                                                   1-1484 5 COO -- 4-(MeOOC)Ph                                                   1-1485 5 COO -- 2-(EtOOC)Ph                                                   1-1486 5 COO -- 4-(EtOOC)Ph                                                   1-1487 5 COO -- 2-(tBuOOC)Ph                                                  1-1488 5 COO -- 4-(tBuOOC)Ph                                                  1-1489 5 COO -- 2-Cl--Ph                                                      1-1490 5 COO -- 4-Cl--Ph                                                      1-1491 5 COO -- 2-Br--Ph                                                      1-1492 5 COO -- 4-Br--Ph                                                      1-1493 5 COO -- 2-I--Ph                                                       1-1494 5 COO -- 4-I--Ph                                                       1-1495 5 COO -- 2-NO.sub.2 --Ph                                               1-1496 5 COO -- 4-NO.sub.2 --Ph                                               1-1497 5 COO -- 2-NH.sub.2 --Ph                                               1-1498 5 COO -- 4-NH.sub.2 --Ph                                               1-1499 5 COO -- 2-(HO.sub.3 S)Ph                                              1-1500 5 COO -- 4-(HO.sub.3 S)Ph                                              1-1501 5 COO -- 2-(NH.sub.2 O.sub.2 S)Ph                                      1-1502 5 COO -- 4-(NH.sub.2 O.sub.2 S)Ph                                      1-1503 5 COO -- 2-CN--Ph                                                      1-1504 5 COO -- 4-CN--Ph                                                      1-1505 5 COO -- 2-(HOCH.sub.2)Ph                                              1-1506 5 COO -- 4-(HOCH.sub.2)Ph                                              1-1507 5 COO -- Me                                                            1-1508 5 COO -- Et                                                            1-1509 5 COO -- Pr                                                            1-1510 5 COO -- iPr                                                           1-1511 5 COO -- Bu                                                            1-1512 5 COO -- HOOCCH.sub.2 --                                               1-1513 5 COO -- HOOC--(CH.sub.2).sub.2 --                                     1-1514 5 COO -- MeCH(COOMe)                                                   1-1515 5 COO -- 1-HOOC-iBu                                                    1-1516 5 COO -- 1-HOOC-iPn                                                    1-1517 5 COO -- Z-1                                                           1-1518 5 COO -- Z-2                                                           1-1519 5 COO -- Z-3                                                           1-1520 5 COO -- Z-4                                                           1-1521 5 COO -- Z-5                                                           1-1522 5 COO -- Z-6                                                           1-1523 5 COO -- Z-7                                                           1-1524 5 COO -- Z-8                                                           1-1525 5 COO -- Z-9                                                           1-1526 5 COO -- Z-10                                                          1-1527 5 COO -- Z-11                                                          1-1528 5 COO -- Z-12                                                          1-1529 5 COO -- 3-Py                                                          1-1530 5 COO -- 4-Py                                                          1-1531 5 CONHCO -- H                                                          1-1532 5 CONHCO -- Ph                                                         1-1533 5 CONHCO -- 2-Me--Ph                                                   1-1534 5 CONHCO -- 4-Me--Ph                                                   1-1535 5 CONHCO -- 2,4-diMe--Ph                                               1-1536 5 CONHCO -- 3,4-diMe--Ph                                               1-1537 5 CONHCO -- 2-(CF.sub.3)Ph                                             1-1538 5 CONHCO -- 4-(CF.sub.3)Ph                                             1-1539 5 CONHCO -- 2-MeOPh                                                    1-1540 5 CONHCO -- 4-MeOPh                                                    1-1541 5 CONHCO -- 2-EtOPh                                                    1-1542 5 CONHCO -- 4-EtOPh                                                    1-1543 5 CONHCO -- 2-HOPh                                                     1-1544 5 CONHCO -- 4-HOPh                                                     1-1545 5 CONHCO -- 2-(HOOC)Ph                                                 1-1546 5 CONHCO -- 4-(HOOC)Ph                                                 1-1547 5 CONHCO -- 2-(MeOOC)Ph                                                1-1548 5 CONHCO -- 4-(MeOOC)Ph                                                1-1549 5 CONHCO -- 2-(EtOOC)Ph                                                1-1550 5 CONHCO -- 4-(EtOOC)Ph                                                1-1551 5 CONHCO -- 2-(tBuOOC)Ph                                               1-1552 5 CONHCO -- 4-(tBuOOC)Ph                                               1-1553 5 CONHCO -- 2-Cl--Ph                                                   1-1554 5 CONHCO -- 4-Cl--Ph                                                   1-1555 5 CONHCO -- 2-Br--Ph                                                   1-1556 5 CONHCO -- 4-Br--Ph                                                   1-1557 5 CONHCO -- 2-I--Ph                                                    1-1558 5 CONHCO -- 4-I--Ph                                                    1-1559 5 CONHCO -- 2-NO.sub.2 --Ph                                            1-1560 5 CONHCO -- 4-NO.sub.2 --Ph                                            1-1561 5 CONHCO -- 2-NH.sub.2 --Ph                                            1-1562 5 CONHCO -- 4-NH.sub.2 --Ph                                            1-1563 5 CONHCO -- 2-(HO.sub.3 S)Ph                                           1-1564 5 CONHCO -- 4-(HO.sub.3 S)Ph                                           1-1565 5 CONHCO -- 2-(NH.sub.2 O.sub.2 S)Ph                                   1-1566 5 CONHCO -- 4-(NH.sub.2 O.sub.2 S)Ph                                   1-1567 5 CONHCO -- 2-CN--Ph                                                   1-1568 5 CONHCO -- 4-CN--Ph                                                   1-1569 5 CONHCO -- 2-(HOCH.sub.2)Ph                                           1-1570 5 CONHCO -- 4-(HOCH.sub.2)Ph                                           1-1571 5 CONHCO -- Me                                                         1-1572 5 CONHCO -- Et                                                         1-1573 5 CONHCO -- Pr                                                         1-1574 5 CONHCO -- iPr                                                        1-1575 5 CONHCO -- Bu                                                         1-1576 5 CONHCO -- HOOCCH.sub.2 --                                            1-1577 5 CONHCO -- MeOOCCH.sub.2 --                                           1-1578 5 CONHCO -- MeCH(COOH)                                                 1-1579 5 CONHCO -- HOOC--(CH.sub.2).sub.2 --                                  1-1580 5 CONHCO -- MeCH(COOMe)                                                1-1581 5 CONHCO -- 1-HOOC-iBu                                                 1-1582 5 CONHCO -- 1-MeOOC-iBu                                                1-1583 5 CONHCO -- 1-HOOC-iPn                                                 1-1584 5 CONHCO -- 1-MeOOC-iPn                                                1-1585 5 CONHCO -- 1-HOOC-2-Me--Bu                                            1-1586 5 CONHCO -- 1-MeOOC-2-Me--Bu                                           1-1587 5 CONHCO -- CH.sub.2 CH.sub.2 SO.sub.3 H                               1-1588 5 CONHCO -- Z-1                                                        1-1589 5 CONHCO -- Z-2                                                        1-1590 5 CONHCO -- Z-3                                                        1-1591 5 CONHCO -- Z-4                                                        1-1592 5 CONHCO -- Z-5                                                        1-1593 5 CONHCO -- Z-6                                                        1-1594 5 CONHCO -- Z-7                                                        1-1595 5 CONHCO -- Z-8                                                        1-1596 5 CONHCO -- Z-9                                                        1-1597 5 CONHCO -- Z-10                                                       1-1598 5 CONHCO -- Z-11                                                       1-1599 5 CONHCO -- Z-12                                                       1-1600 5 CONHCO -- 3-Py                                                       1-1601 5 CONHCO -- 4-Py                                                       1-1602 5 CON(Ac)CO -- H                                                       1-1603 5 CON(Ac)CO -- Ph                                                      1-1604 5 CON(Ac)CO -- 2-Me--Ph                                                1-1605 5 CON(Ac)CO -- 4-Me--Ph                                                1-1606 5 CON(Ac)CO -- 2,4-diMe--Ph                                            1-1607 5 CON(Ac)CO -- 3,4-diMe--Ph                                            1-1608 5 CON(Ac)CO -- 2-(CF.sub.3)Ph                                          1-1609 5 CON(Ac)CO -- 4-(CF.sub.3)Ph                                          1-1610 5 CON(Ac)CO -- 2-MeOPh                                                 1-1611 5 CON(Ac)CO -- 4-MeOPh                                                 1-1612 5 CON(Ac)CO -- 2-EtOPh                                                 1-1613 5 CON(Ac)CO -- 4-EtOPh                                                 1-1614 5 CON(Ac)CO -- 2-HOPh                                                  1-1615 5 CON(Ac)CO -- 4-HOPh                                                  1-1616 5 CON(Ac)CO -- 2-(HOOC)Ph                                              1-1617 5 CON(Ac)CO -- 4-(HOOC)Ph                                              1-1618 5 CON(Ac)CO -- 2-(MeOOC)Ph                                             1-1619 5 CON(Ac)CO -- 4-(MeOOC)Ph                                             1-1620 5 CON(Ac)CO -- 2-(EtOOC)Ph                                             1-1621 5 CON(Ac)CO -- 4-(EtOOC)Ph                                             1-1622 5 CON(Ac)CO -- 2-(tBuOOC)Ph                                            1-1623 5 CON(Ac)CO -- 4-(tBuOOC)Ph                                            1-1624 5 CON(Ac)CO -- 2-Cl--Ph                                                1-1625 5 CON(Ac)CO -- 4-Cl--Ph                                                1-1626 5 CON(Ac)CO -- 2-Br--Ph                                                1-1627 5 CON(Ac)CO -- 4-Br--Ph                                                1-1628 5 CON(Ac)CO -- 2-I--Ph                                                 1-1629 5 CON(Ac)CO -- 4-I--Ph                                                 1-1630 5 CON(Ac)CO -- 2-NO.sub.2 --Ph                                         1-1631 5 CON(Ac)CO -- 4-NO.sub.2 --Ph                                         1-1632 5 CON(Ac)CO -- 2-NH.sub.2 --Ph                                         1-1633 5 CON(Ac)CO -- 4-NH.sub.2 --Ph                                         1-1634 5 CON(Ac)CO -- 2-(HO.sub.3 S)Ph                                        1-1635 5 CON(Ac)CO -- 4-(HO.sub.3 S)Ph                                        1-1636 5 CON(Ac)CO -- 2-(NH.sub.2 O.sub.2 S)Ph                                1-1637 5 CON(Ac)CO -- 4-(NH.sub.2 O.sub.2 S)Ph                                1-1638 5 CON(Ac)CO -- 2-CN--Ph                                                1-1639 5 CON(Ac)CO -- 4-CN--Ph                                                1-1640 5 CON(Ac)CO -- 2-(HOCH.sub.2)Ph                                        1-1641 5 CON(Ac)CO -- 4-(HOCH.sub.2)Ph                                        1-1642 5 CON(Ac)CO -- Me                                                      1-1643 5 CON(Ac)CO -- Et                                                      1-1644 5 CON(Ac)CO -- Pr                                                      1-1645 5 CON(Ac)CO -- iPr                                                     1-1646 5 CON(Ac)CO -- Bu                                                      1-1647 5 CON(Ac)CO -- HOOCCH.sub.2 --                                         1-1648 5 CON(Ac)CO -- MeOOCCH.sub.2 --                                        1-1649 5 CON(Ac)CO -- MeCH(COOH)                                              1-1650 5 CON(Ac)CO -- HOOC--(CH.sub.2).sub.2 --                               1-1651 5 CON(Ac)CO -- MeCH(COOMe)                                             1-1652 5 CON(Ac)CO -- 1-HOOC-iBu                                              1-1653 5 CON(Ac)CO -- 1-MeOOC-iBu                                             1-1654 5 CON(Ac)CO -- 1-HOOC-iPn                                              1-1655 5 CON(Ac)CO -- 1-MeOOC-iPn                                             1-1656 5 CON(Ac)CO -- 1-HOOC-2-Me--Bu                                         1-1657 5 CON(Ac)CO -- 1-MeOOC-2-Me--Bu                                        1-1658 5 CON(Ac)CO -- CH.sub.2 CH.sub.2 SO.sub.3 H                            1-1659 5 CON(Ac)CO -- Z-1                                                     1-1660 5 CON(Ac)CO -- Z-2                                                     1-1661 5 CON(Ac)CO -- Z-3                                                     1-1662 5 CON(Ac)CO -- Z-4                                                     1-1663 5 CON(Ac)CO -- Z-5                                                     1-1664 5 CON(Ac)CO -- Z-6                                                     1-1665 5 CON(Ac)CO -- Z-7                                                     1-1666 5 CON(Ac)CO -- Z-8                                                     1-1667 5 CON(Ac)CO -- Z-9                                                     1-1668 5 CON(Ac)CO -- Z-10                                                    1-1669 5 CON(Ac)CO -- Z-11                                                    1-1670 5 CON(Ac)CO -- Z-12                                                    1-1671 5 CON(Ac)CO -- 3-Py                                                    1-1672 5 CON(Ac)CO -- 4-Py                                                    1-1673 5 CONHCO NH H                                                          1-1674 5 CONHCO NH Ph                                                         1-1675 5 CONHCO NH 2-Me--Ph                                                   1-1676 5 CONHCO NH 4-Me--Ph                                                   1-1677 5 CONHCO NH 2,4-diMe--Ph                                               1-1678 5 CONHCO NH 3,4-diMe--Ph                                               1-1679 5 CONHCO NH 2-(CF.sub.3)Ph                                             1-1680 5 CONHCO NH 4-(CF.sub.3)Ph                                             1-1681 5 CONHCO NH 2-MeOPh                                                    1-1682 5 CONHCO NH 4-MeOPh                                                    1-1683 5 CONHCO NH 2-EtOPh                                                    1-1684 5 CONHCO NH 4-EtOPh                                                    1-1685 5 CONHCO NH 2-HOPh                                                     1-1686 5 CONHCO NH 4-HOPh                                                     1-1687 5 CONHCO NH 2-(HOOC)Ph                                                 1-1688 5 CONHCO NH 4-(HOOC)Ph                                                 1-1689 5 CONHCO NH 2-(MeOOC)Ph                                                1-1690 5 CONHCO NH 4-(MeOOC)Ph                                                1-1691 5 CONHCO NH 2-(EtOOC)Ph                                                1-1692 5 CONHCO NH 4-(EtOOC)Ph                                                1-1693 5 CONHCO NH 2-(tBuOOC)Ph                                               1-1694 5 CONHCO NH 4-(tBuOOC)Ph                                               1-1695 5 CONHCO NH 2-Cl--Ph                                                   1-1696 5 CONHCO NH 4-Cl--Ph                                                   1-1697 5 CONHCO NH 2-Br--Ph                                                   1-1698 5 CONHCO NH 4-Br--Ph                                                   1-1699 5 CONHCO NH 2-I--Ph                                                    1-1700 5 CONHCO NH 4-I--Ph                                                    1-1701 5 CONHCO NH 2-NO.sub.2 --Ph                                            1-1702 5 CONHCO NH 4-NO.sub.2 --Ph                                            1-1703 5 CONHCO NH 2-NH.sub.2 --Ph                                            1-1704 5 CONHCO NH 4-NH.sub.2 --Ph                                            1-1705 5 CONHCO NH 2-(HO.sub.3 S)Ph                                           1-1706 5 CONHCO NH 4-(HO.sub.3 S)Ph                                           1-1707 5 CONHCO NH 2-(NH.sub.2 O.sub.2 S)Ph                                   1-1708 5 CONHCO NH 4-(NH.sub.2 O.sub.2 S)Ph                                   1-1709 5 CONHCO NH 2-CN--Ph                                                   1-1710 5 CONHCO NH 4-CN--Ph                                                   1-1711 5 CONHCO NH 2-(HOCH.sub.2)Ph                                           1-1712 5 CONHCO NH 4-(HOCH.sub.2)Ph                                           1-1713 5 CONHCO NH Me                                                         1-1714 5 CONHCO NH Et                                                         1-1715 5 CONHCO NH Pr                                                         1-1716 5 CONHCO NH iPr                                                        1-1717 5 CONHCO NH Bu                                                         1-1718 5 CONHCO NH HOOCCH.sub.2 --                                            1-1719 5 CONHCO NH MeOOCCH.sub.2 --                                           1-1720 5 CONHCO NH MeCH(COOH)                                                 1-1721 5 CONHCO NH HOOC--(CH.sub.2).sub.2 --                                  1-1722 5 CONHCO NH MeCH(COOMe)                                                1-1723 5 CONHCO NH 1-HOOC-iBu                                                 1-1724 5 CONHCO NH 1-MeOOC-iBu                                                1-1725 5 CONHCO NH 1-HOOC-iPn                                                 1-1726 5 CONHCO NH 1-MeOOC-iPn                                                1-1727 5 CONHCO NH 1-HOOC-2-Me--Bu                                            1-1728 5 CONHCO NH 1-MeOOC-2-Me--Bu                                           1-1729 5 CONHCO NH CH.sub.2 CH.sub.2 SO.sub.3 H                               1-1730 5 CONHCO NH HO                                                         1-1731 5 CONHCO NH MeO                                                        1-1732 5 CONHCO NH EtO                                                        1-1733 5 CONHCO NH PrO                                                        1-1734 5 CONHCO NH iPrO                                                       1-1735 5 CONHCO NH BuO                                                        1-1736 5 CONHCO NH iBuO                                                       1-1737 5 CONHCO NH sBuO                                                       1-1738 5 CONHCO NH tBuO                                                       1-1739 5 CONHCO NH HxO                                                        1-1740 5 CONHCO NH PhO                                                        1-1741 5 CONHCO NH BzO                                                        1-1742 5 CONHCO NH Z-1                                                        1-1743 5 CONHCO NH Z-2                                                        1-1744 5 CONHCO NH Z-3                                                        1-1745 5 CONHCO NH Z-4                                                        1-1746 5 CONHCO NH Z-5                                                        1-1747 5 CONHCO NH Z-6                                                        1-1748 5 CONHCO NH Z-7                                                        1-1749 5 CONHCO NH Z-8                                                        1-1750 5 CONHCO NH Z-9                                                        1-1751 5 CONHCO NH Z-10                                                       1-1752 5 CONHCO NH Z-11                                                       1-1753 5 CONHCO NH Z-12                                                       1-1754 5 CONHCO NH 3-Py                                                       1-1755 5 CONHCO NH 4-Py                                                       1-1756 5 CONHSO.sub.2 -- H                                                    1-1757 5 CONHSO.sub.2 -- Ph                                                   1-1758 5 CONHSO.sub.2 -- 2-Me--Ph                                             1-1759 5 CONHSO.sub.2 -- 4-Me--Ph                                             1-1760 5 CONHSO.sub.2 -- 2,4-diMe--Ph                                         1-1761 5 CONHSO.sub.2 -- 3,4-diMe--Ph                                         1-1762 5 CONHSO.sub.2 -- 2-(CF.sub.3)Ph                                       1-1763 5 CONHSO.sub.2 -- 4-(CF.sub.3)Ph                                       1-1764 5 CONHSO.sub.2 -- 2-MeOPh                                              1-1765 5 CONHSO.sub.2 -- 4-MeOPh                                              1-1766 5 CONHSO.sub.2 -- 2-EtOPh                                              1-1767 5 CONHSO.sub.2 -- 4-EtOPh                                              1-1768 5 CONHSO.sub.2 -- 2-HOPh                                               1-1769 5 CONHSO.sub.2 -- 4-HOPh                                               1-1770 5 CONHSO.sub.2 -- 2-(HOOC)Ph                                           1-1771 5 CONHSO.sub.2 -- 4-(HOOC)Ph                                           1-1772 5 CONHSO.sub.2 -- 2-(MeOOC)Ph                                          1-1773 5 CONHSO.sub.2 -- 4-(MeOOC)Ph                                          1-1774 5 CONHSO.sub.2 -- 2-(EtOOC)Ph                                          1-1775 5 CONHSO.sub.2 -- 4-(EtOOC)Ph                                          1-1776 5 CONHSO.sub.2 -- 2-(tBuOOC)Ph                                         1-1777 5 CONHSO.sub.2 -- 4-(tBuOOC)Ph                                         1-1778 5 CONHSO.sub.2 -- 2-Cl--Ph                                             1-1779 5 CONHSO.sub.2 -- 4-Cl--Ph                                             1-1780 5 CONHSO.sub.2 -- 2-Br--Ph                                             1-1781 5 CONHSO.sub.2 -- 4-Br--Ph                                             1-1782 5 CONHSO.sub.2 -- 2-I--Ph                                              1-1783 5 CONHSO.sub.2 -- 4-I--Ph                                              1-1784 5 CONHSO.sub.2 -- 2-NO.sub.2 --Ph                                      1-1785 5 CONHSO.sub.2 -- 4-NO.sub.2 --Ph                                      1-1786 5 CONHSO.sub.2 -- 2-NH.sub.2 --Ph                                      1-1787 5 CONHSO.sub.2 -- 4-NH.sub.2 --Ph                                      1-1788 5 CONHSO.sub.2 -- 2-(HO.sub.3 S)Ph                                     1-1789 5 CONHSO.sub.2 -- 4-(HO.sub.3 S)Ph                                     1-1790 5 CONHSO.sub.2 -- 2-(NH.sub.2 O.sub.2 S)Ph                             1-1791 5 CONHSO.sub.2 -- 4-(NH.sub.2 O.sub.2 S)Ph                             1-1792 5 CONHSO.sub.2 -- 2-CN--Ph                                             1-1793 5 CONHSO.sub.2 -- 4-CN--Ph                                             1-1794 5 CONHSO.sub.2 -- 2-(HOCH.sub.2)Ph                                     1-1795 5 CONHSO.sub.2 -- 4-(HOCH.sub.2)Ph                                     1-1796 5 CONHSO.sub.2 -- Me                                                   1-1797 5 CONHSO.sub.2 -- Et                                                   1-1798 5 CONHSO.sub.2 -- Pr                                                   1-1799 5 CONHSO.sub.2 -- iPr                                                  1-1800 5 CONHSO.sub.2 -- Bu                                                   1-1801 5 CONHSO.sub.2 -- HOOCCH.sub.2 --                                      1-1802 5 CONHSO.sub.2 -- MeOOCCH.sub.2 --                                     1-1803 5 CONHSO.sub.2 -- MeCH(COOH)                                           1-1804 5 CONHSO.sub.2 -- HOOC--(CH.sub.2).sub.2 --                            1-1805 5 CONHSO.sub.2 -- MeCH(COOMe)                                          1-1806 5 CONHSO.sub.2 -- 1-HOOC-iBu                                           1-1807 5 CONHSO.sub.2 -- 1-MeOOC-iBu                                          1-1808 5 CONHSO.sub.2 -- 1-HOOC-iPn                                           1-1809 5 CONHSO.sub.2 -- 1-MeOOC-iPn                                          1-1810 5 CONHSO.sub.2 -- 1-HOOC-2-Me--Bu                                      1-1811 5 CONHSO.sub.2 -- 1-MeOOC-2-Me--Bu                                     1-1812 5 CONHSO.sub.2 -- CH.sub.2 CH.sub.2 SO.sub.3 H                         1-1813 5 CONHSO.sub.2 -- OH                                                   1-1814 5 CONHSO.sub.2 -- MeO                                                  1-1815 5 CONHSO.sub.2 -- EtO                                                  1-1816 5 CONHSO.sub.2 -- PrO                                                  1-1817 5 CONHSO.sub.2 -- iPrO                                                 1-1818 5 CONHSO.sub.2 -- BuO                                                  1-1819 5 CONHSO.sub.2 -- iBuO                                                 1-1820 5 CONHSO.sub.2 -- sBuO                                                 1-1821 5 CONHSO.sub.2 -- tBuO                                                 1-1822 5 CONHSO.sub.2 -- HxO                                                  1-1823 5 CONHSO.sub.2 -- PhO                                                  1-1824 5 CONHSO.sub.2 -- BzO                                                  1-1825 5 CONHSO.sub.2 -- Z-1                                                  1-1826 5 CONHSO.sub.2 -- Z-2                                                  1-1827 5 CONHSO.sub.2 -- Z-3                                                  1-1828 5 CONHSO.sub.2 -- Z-4                                                  1-1829 5 CONHSO.sub.2 -- Z-5                                                  1-1830 5 CONHSO.sub.2 -- Z-6                                                  1-1831 5 CONHSO.sub.2 -- Z-7                                                  1-1832 5 CONHSO.sub.2 -- Z-8                                                  1-1833 5 CONHSO.sub.2 -- Z-9                                                  1-1834 5 CONHSO.sub.2 -- Z-10                                                 1-1835 5 CONHSO.sub.2 -- Z-11                                                 1-1836 5 CONHSO.sub.2 -- Z-12                                                 1-1837 5 CONHSO.sub.2 -- 3-Py                                                 1-1838 5 CONHSO.sub.2 -- 4-Py                                                 1-1839 5 CONHSO.sub.2 NH H                                                    1-1840 5 CONHSO.sub.2 NH Ph                                                   1-1841 5 CONHSO.sub.2 NH 2-Me--Ph                                             1-1842 5 CONHSO.sub.2 NH 4-Me--Ph                                             1-1843 5 CONHSO.sub.2 NH 2,4-diMe--Ph                                         1-1844 5 CONHSO.sub.2 NH 3,4-diMe--Ph                                         1-1845 5 CONHSO.sub.2 NH 2-(CF.sub.3)Ph                                       1-1846 5 CONHSO.sub.2 NH 4-(CF.sub.3)Ph                                       1-1847 5 CONHSO.sub.2 NH 2-MeOPh                                              1-1848 5 CONHSO.sub.2 NH 4-MeOPh                                              1-1849 5 CONHSO.sub.2 NH 2-EtOPh                                              1-1850 5 CONHSO.sub.2 NH 4-EtOPh                                              1-1851 5 CONHSO.sub.2 NH 2-HOPh                                               1-1852 5 CONHSO.sub.2 NH 4-HOPh                                               1-1853 5 CONHSO.sub.2 NH 2-(HOOC)Ph                                           1-1854 5 CONHSO.sub.2 NH 4-(HOOC)Ph                                           1-1855 5 CONHSO.sub.2 NH 2-(MeOOC)Ph                                          1-1856 5 CONHSO.sub.2 NH 4-(MeOOC)Ph                                          1-1857 5 CONHSO.sub.2 NH 2-(EtOOC)Ph                                          1-1858 5 CONHSO.sub.2 NH 4-(EtOOC)Ph                                          1-1859 5 CONHSO.sub.2 NH 2-(tBuOOC)Ph                                         1-1860 5 CONHSO.sub.2 NH 4-(tBuOOC)Ph                                         1-1861 5 CONHSO.sub.2 NH 2-Cl--Ph                                             1-1862 5 CONHSO.sub.2 NH 4-Cl--Ph                                             1-1863 5 CONHSO.sub.2 NH 2-Br--Ph                                             1-1864 5 CONHSO.sub.2 NH 4-Br--Ph                                             1-1865 5 CONHSO.sub.2 NH 2-I--Ph                                              1-1866 5 CONHSO.sub.2 NH 4-I--Ph                                              1-1867 5 CONHSO.sub.2 NH 2-NO.sub.2 --Ph                                      1-1868 5 CONHSO.sub.2 NH 4-NO.sub.2 --Ph                                      1-1869 5 CONHSO.sub.2 NH 2-NH.sub.2 --Ph                                      1-1870 5 CONHSO.sub.2 NH 4-NH.sub.2 --Ph                                      1-1871 5 CONHSO.sub.2 NH 2-(HO.sub.3 S)Ph                                     1-1872 5 CONHSO.sub.2 NH 4-(HO.sub.3 S)Ph                                     1-1873 5 CONHSO.sub.2 NH 2-(NH.sub.2 O.sub.2 S)Ph                             1-1874 5 CONHSO.sub.2 NH 4-(NH.sub.2 O.sub.2 S)Ph                             1-1875 5 CONHSO.sub.2 NH 2-CN--Ph                                             1-1876 5 CONHSO.sub.2 NH 4-CN--Ph                                             1-1877 5 CONHSO.sub.2 NH 2-(HOCH.sub.2)Ph                                     1-1878 5 CONHSO.sub.2 NH 4-(HOCH.sub.2)Ph                                     1-1879 5 CONHSO.sub.2 NH Me                                                   1-1880 5 CONHSO.sub.2 NH Et                                                   1-1881 5 CONHSO.sub.2 NH Pr                                                   1-1882 5 CONHSO.sub.2 NH iPr                                                  1-1883 5 CONHSO.sub.2 NH Bu                                                   1-1884 5 CONHSO.sub.2 NH HOOCCH.sub.2 --                                      1-1885 5 CONHSO.sub.2 NH MeOOCCH.sub.2 --                                     1-1886 5 CONHSO.sub.2 NH MeCH(COOH)                                           1-1887 5 CONHSO.sub.2 NH HOOC--(CH.sub.2).sub.2 --                            1-1888 5 CONHSO.sub.2 NH MeCH(COOMe)                                          1-1889 5 CONHSO.sub.2 NH 1-HOOC-iBu                                           1-1890 5 CONHSO.sub.2 NH 1-MeOOC-iBu                                          1-1891 5 CONHSO.sub.2 NH 1-HOOC-iPn                                           1-1892 5 CONHSO.sub.2 NH 1-MeOOC-iPn                                          1-1893 5 CONHSO.sub.2 NH 1-HOOC-2-Me--Bu                                      1-1894 5 CONHSO.sub.2 NH 1-MeOOC-2-Me--Bu                                     1-1895 5 CONHSO.sub.2 NH CH.sub.2 CH.sub.2 SO.sub.3 H                         1-1896 5 CONHSO.sub.2 NH OH                                                   1-1897 5 CONHSO.sub.2 NH MeO                                                  1-1898 5 CONHSO.sub.2 NH EtO                                                  1-1899 5 CONHSO.sub.2 NH PrO                                                  1-1900 5 CONHSO.sub.2 NH iPrO                                                 1-1901 5 CONHSO.sub.2 NH BuO                                                  1-1902 5 CONHSO.sub.2 NH iBuO                                                 1-1903 5 CONHSO.sub.2 NH sBuO                                                 1-1904 5 CONHSO.sub.2 NH tBuO                                                 1-1905 5 CONHSO.sub.2 NH HxO                                                  1-1906 5 CONHSO.sub.2 NH PhO                                                  1-1907 5 CONHSO.sub.2 NH BzO                                                  1-1908 5 CONHSO.sub.2 NH Z-1                                                  1-1909 5 CONHSO.sub.2 NH Z-2                                                  1-1910 5 CONHSO.sub.2 NH Z-3                                                  1-1911 5 CONHSO.sub.2 NH Z-4                                                  1-1912 5 CONHSO.sub.2 NH Z-5                                                  1-1913 5 CONHSO.sub.2 NH Z-6                                                  1-1914 5 CONHSO.sub.2 NH Z-7                                                  1-1915 5 CONHSO.sub.2 NH Z-8                                                  1-1916 5 CONHSO.sub.2 NH Z-9                                                  1-1917 5 CONHSO.sub.2 NH Z-10                                                 1-1918 5 CONHSO.sub.2 NH Z-11                                                 1-1919 5 CONHSO.sub.2 NH Z-12                                                 1-1920 5 CONHSO.sub.2 NH 3-Py                                                 1-1921 5 CONHSO.sub.2 NH 4-Py                                                 1-1922 5 NHCO -- H                                                            1-1923 5 NHCO -- Ph                                                           1-1924 5 NHCO -- 2-Me--Ph                                                     1-1925 5 NHCO -- 4-Me--Ph                                                     1-1926 5 NHCO -- 2,4-diMe--Ph                                                 1-1927 5 NHCO -- 3,4-diMe--Ph                                                 1-1928 5 NHCO -- 2-(CF.sub.3)Ph                                               1-1929 5 NHCO -- 4-(CF.sub.3)Ph                                               1-1930 5 NHCO -- 2-MeOPh                                                      1-1931 5 NHCO -- 4-MeOPh                                                      1-1932 5 NHCO -- 2-EtOPh                                                      1-1933 5 NHCO -- 4-EtOPh                                                      1-1934 5 NHCO -- 2-HOPh                                                       1-1935 5 NHCO -- 4-HOPh                                                       1-1936 5 NHCO -- 2-(HOOC)Ph                                                   1-1937 5 NHCO -- 4-(HOOC)Ph                                                   1-1938 5 NHCO -- 2-(MeOOC)Ph                                                  1-1939 5 NHCO -- 4-(MeOOC)Ph                                                  1-1940 5 NHCO -- 2-(EtOOC)Ph                                                  1-1941 5 NHCO -- 4-(EtOOC)Ph                                                  1-1942 5 NHCO -- 2-(tBuOOC)Ph                                                 1-1943 5 NHCO -- 4-(tBuOOC)Ph                                                 1-1944 5 NHCO -- 2-Cl--Ph                                                     1-1945 5 NHCO -- 4-Cl--Ph                                                     1-1946 5 NHCO -- 2-Br--Ph                                                     1-1947 5 NHCO -- 4-Br--Ph                                                     1-1948 5 NHCO -- 2-I--Ph                                                      1-1949 5 NHCO -- 4-I--Ph                                                      1-1950 5 NHCO -- 2-NO.sub.2 --Ph                                              1-1951 5 NHCO -- 4-NO.sub.2 --Ph                                              1-1952 5 NHCO -- 2-NH.sub.2 --Ph                                              1-1953 5 NHCO -- 4-NH.sub.2 --Ph                                              1-1954 5 NHCO -- 2-(HO.sub.3 S)Ph                                             1-1955 5 NHCO -- 4-(HO.sub.3 S)Ph                                             1-1956 5 NHCO -- 2-(NH.sub.2 O.sub.2 S)Ph                                     1-1957 5 NHCO -- 4-(NH.sub.2 O.sub.2 S)Ph                                     1-1958 5 NHCO -- 2-CN--Ph                                                     1-1959 5 NHCO -- 4-CN--Ph                                                     1-1960 5 NHCO -- 2-(HOCH.sub.2)Ph                                             1-1961 5 NHCO -- 4-(HOCH.sub.2)Ph                                             1-1962 5 NHCO -- Me                                                           1-1963 5 NHCO -- Et                                                           1-1964 5 NHCO -- Pr                                                           1-1965 5 NHCO -- iPr                                                          1-1966 5 NHCO -- Bu                                                           1-1967 5 NHCO -- HOOC--(CH.sub.2).sub.2 --                                    1-1968 5 NHCO -- MeOOCCH.sub.2 --                                             1-1969 5 NHCO -- MeCH(COOH)                                                   1-1970 5 NHCO -- HOOC--(CH.sub.2).sub.2 --                                    1-1971 5 NHCO -- MeCH(COOMe)                                                  1-1972 5 NHCO -- 1-HOOC-iBu                                                   1-1973 5 NHCO -- 1-HOOC-iPn                                                   1-1974 5 NHCO -- 1-HOOC-2-Me--Bu                                              1-1975 5 NHCO -- CH.sub.2 CH.sub.2 SO.sub.3 H                                 1-1976 5 NHCO -- MeO                                                          1-1977 5 NHCO -- EtO                                                          1-1978 5 NHCO -- PrO                                                          1-1979 5 NHCO -- Z-1                                                          1-1980 5 NHCO -- Z-2                                                          1-1981 5 NHCO -- Z-3                                                          1-1982 5 NHCO -- Z-4                                                          1-1983 5 NHCO -- Z-5                                                          1-1984 5 NHCO -- Z-6                                                          1-1985 5 NHCO -- Z-7                                                          1-1986 5 NHCO -- Z-8                                                          1-1987 5 NHCO -- Z-9                                                          1-1988 5 NHCO -- Z-10                                                         1-1989 5 NHCO -- Z-11                                                         1-1990 5 NHCO -- Z-12                                                         1-1991 5 NHCO -- 3-Py                                                         1-1992 5 NHCO -- 4-Py                                                         1-1993 5 NHCO NH H                                                            1-1994 5 NHCO NH Ph                                                           1-1995 5 NHCO NH 2-Me--Ph                                                     1-1996 5 NHCO NH 4-Me--Ph                                                     1-1997 5 NHCO NH 2,4-diMe--Ph                                                 1-1998 5 NHCO NH 3,4-diMe--Ph                                                 1-1999 5 NHCO NH 2-(CF.sub.3)Ph                                               1-2000 5 NHCO NH 4-(CF.sub.3)Ph                                               1-2001 5 NHCO NH 2-MeOPh                                                      1-2002 5 NHCO NH 4-MeOPh                                                      1-2003 5 NHCO NH 2-EtOPh                                                      1-2004 5 NHCO NH 4-EtOPh                                                      1-2005 5 NHCO NH 2-HOPh                                                       1-2006 5 NHCO NH 4-HOPh                                                       1-2007 5 NHCO NH 2-(HOOC)Ph                                                   1-2008 5 NHCO NH 4-(HOOC)Ph                                                   1-2009 5 NHCO NH 2-(MeOOC)Ph                                                  1-2010 5 NHCO NH 4-(MeOOC)Ph                                                  1-2011 5 NHCO NH 2-(EtOOC)Ph                                                  1-2012 5 NHCO NH 4-(EtOOC)Ph                                                  1-2013 5 NHCO NH 2-(tBuOOC)Ph                                                 1-2014 5 NHCO NH 4-(tBuOOC)Ph                                                 1-2015 5 NHCO NH 2-Cl--Ph                                                     1-2016 5 NHCO NH 4-Cl--Ph                                                     1-2017 5 NHCO NH 2-Br--Ph                                                     1-2018 5 NHCO NH 4-Br--Ph                                                     1-2019 5 NHCO NH 2-I--Ph                                                      1-2020 5 NHCO NH 4-I--Ph                                                      1-2021 5 NHCO NH 2-NO.sub.2 --Ph                                              1-2022 5 NHCO NH 4-NO.sub.2 --Ph                                              1-2023 5 NHCO NH 2-NH.sub.2 --Ph                                              1-2024 5 NHCO NH 4-NH.sub.2 --Ph                                              1-2025 5 NHCO NH 2-(HO.sub.3 S)Ph                                             1-2026 5 NHCO NH 4-(HO.sub.3 S)Ph                                             1-2027 5 NHCO NH 2-(NH.sub.2 O.sub.2 S)Ph                                     1-2028 5 NHCO NH 4-(NH.sub.2 O.sub.2 S)Ph                                     1-2029 5 NHCO NH 2-CN--Ph                                                     1-2030 5 NHCO NH 4-CN--Ph                                                     1-2031 5 NHCO NH 2-(HOCH.sub.2)Ph                                             1-2032 5 NHCO NH 4-(HOCH.sub.2)Ph                                             1-2033 5 NHCO NH Me                                                           1-2034 5 NHCO NH Et                                                           1-2035 5 NHCO NH Pr                                                           1-2036 5 NHCO NH iPr                                                          1-2037 5 NHCO NH Bu                                                           1-2038 5 NHCO NH HOOCCH.sub.2 --                                              1-2039 5 NHCO NH MeOOCCH.sub.2 --                                             1-2040 5 NHCO NH MeCH(COOH)                                                   1-2041 5 NHCO NH HOOC--(CH.sub.2).sub.2 --                                    1-2042 5 NHCO NH MeCH(COOMe)                                                  1-2043 5 NHCO NH 1-HOOC-iBu                                                   1-2044 5 NHCO NH 1-MeOOC-iBu                                                  1-2045 5 NHCO NH 1-HOOC-iPn                                                   1-2046 5 NHCO NH 1-MeOOC-iPn                                                  1-2047 5 NHCO NH 1-HOOC-2-Me--Bu                                              1-2048 5 NHCO NH 1-MeOOC-2-Me--Bu                                             1-2049 5 NHCO NH CH.sub.2 CH.sub.2 SO.sub.3 H                                 1-2050 5 NHCO NH OH                                                           1-2051 5 NHCO NH MeO                                                          1-2052 5 NHCO NH EtO                                                          1-2053 5 NHCO NH PrO                                                          1-2054 5 NHCO NH iPrO                                                         1-2055 5 NHCO NH BuO                                                          1-2056 5 NHCO NH iBuO                                                         1-2057 5 NHCO NH sBuO                                                         1-2058 5 NHCO NH tBuO                                                         1-2059 5 NHCO NH HxO                                                          1-2060 5 NHCO NH PhO                                                          1-2061 5 NHCO NH BzO                                                          1-2062 5 NHCO NH Z-1                                                          1-2063 5 NHCO NH Z-2                                                          1-2064 5 NHCO NH Z-3                                                          1-2065 5 NHCO NH Z-4                                                          1-2066 5 NHCO NH Z-5                                                          1-2067 5 NHCO NH Z-6                                                          1-2068 5 NHCO NH Z-7                                                          1-2069 5 NHCO NH Z-8                                                          1-2070 5 NHCO NH Z-9                                                          1-2071 5 NHCO NH Z-10                                                         1-2072 5 NHCO NH Z-11                                                         1-2073 5 NHCO NH Z-12                                                         1-2074 5 NHCO NH 3-Py                                                         1-2075 5 NHCO NH 4-Py                                                         1-2076 5 NHCO NMe Ph                                                          1-2077 5 NHCO NMe 2-Me--Ph                                                    1-2078 5 NHCO NMe 4-Me--Ph                                                    1-2079 5 NHCO NMe 2,4-diMe--Ph                                                1-2080 5 NHCO NMe 3,4-diMe--Ph                                                1-2081 5 NHCO NMe 2-(CF.sub.3)Ph                                              1-2082 5 NHCO NMe 4-(CF.sub.3)Ph                                              1-2083 5 NHCO NMe 2-MeOPh                                                     1-2084 5 NHCO NMe 4-MeOPh                                                     1-2085 5 NHCO NMe 2-EtOPh                                                     1-2086 5 NHCO NMe 4-EtOPh                                                     1-2087 5 NHCO NMe 2-HOPh                                                      1-2088 5 NHCO NMe 4-HOPh                                                      1-2089 5 NHCO NMe 2-(HOOC)Ph                                                  1-2090 5 NHCO NMe 4-(HOOC)Ph                                                  1-2091 5 NHCO NMe 2-(MeOOC)Ph                                                 1-2092 5 NHCO NMe 4-(MeOOC)Ph                                                 1-2093 5 NHCO NMe 2-(EtOOC)Ph                                                 1-2094 5 NHCO NMe 4-(EtOOC)Ph                                                 1-2095 5 NHCO NMe 2-(tBuOOC)Ph                                                1-2096 5 NHCO NMe 4-(tBuOOC)Ph                                                1-2097 5 NHCO NMe 2-Cl--Ph                                                    1-2098 5 NHCO NMe 4-Cl--Ph                                                    1-2099 5 NHCO NMe 2-Br--Ph                                                    1-2100 5 NHCO NMe 4-Br--Ph                                                    1-2101 5 NHCO NMe 2-I--Ph                                                     1-2102 5 NHCO NMe 4-I--Ph                                                     1-2103 5 NHCO NMe 2-NO.sub.2 --Ph                                             1-2104 5 NHCO NMe 4-NO.sub.2 --Ph                                             1-2105 5 NHCO NMe 2-NH.sub.2 --Ph                                             1-2106 5 NHCO NMe 4-NH.sub.2 --Ph                                             1-2107 5 NHCO NMe 2-(HO.sub.3 S)Ph                                            1-2108 5 NHCO NMe 4-(HO.sub.3 S)Ph                                            1-2109 5 NHCO NMe 2-(NH.sub.2 O.sub.2 S)Ph                                    1-2110 5 NHCO NMe 4-(NH.sub.2 O.sub.2 S)Ph                                    1-2111 5 NHCO NMe 2-CN--Ph                                                    1-2112 5 NHCO NMe 4-CN--Ph                                                    1-2113 5 NHCO NMe 2-(HOCH.sub.2)Ph                                            1-2114 5 NHCO NMe 4-(HOCH.sub.2)Ph                                            1-2115 5 NHCO NMe Me                                                          1-2116 5 NHCO NMe Et                                                          1-2117 5 NHCO NMe Pr                                                          1-2118 5 NHCO NMe iPr                                                         1-2119 5 NHCO NMe Bu                                                          1-2120 5 NHCO NMe HOOCCH.sub.2 --                                             1-2121 5 NHCO NMe MeOOCCH.sub.2 --                                            1-2122 5 NHCO NMe MeCH(COOH)                                                  1-2123 5 NHCO NMe HOOC--(CH.sub.2).sub.2 --                                   1-2124 5 NHCO NMe MeCH(COOMe)                                                 1-2125 5 NHCO NMe 1-HOOC-iBu                                                  1-2126 5 NHCO NMe 1-MeOOC-iBu                                                 1-2127 5 NHCO NMe 1-HOOC-iPn                                                  1-2128 5 NHCO NMe 1-MeOOC-iPn                                                 1-2129 5 NHCO NMe 1-HOOC-2-Me--Bu                                             1-2130 5 NHCO NMe 1-MeOOC-2-Me--Bu                                            1-2131 5 NHCO NMe CH.sub.2 CH.sub.2 SO.sub.3 H                                1-2132 5 NHCO NMe OH                                                          1-2133 5 NHCO NMe MeO                                                         1-2134 5 NHCO NMe EtO                                                         1-2135 5 NHCO NMe PrO                                                         1-2136 5 NHCO NMe iPrO                                                        1-2137 5 NHCO NMe BuO                                                         1-2138 5 NHCO NMe iBuO                                                        1-2139 5 NHCO NMe sBuO                                                        1-2140 5 NHCO NMe tBuO                                                        1-2141 5 NHCO NMe HxO                                                         1-2142 5 NHCO NMe PhO                                                         1-2143 5 NHCO NMe BzO                                                         1-2144 5 NHCO NMe Z-1                                                         1-2145 5 NHCO NMe Z-2                                                         1-2146 5 NHCO NMe Z-3                                                         1-2147 5 NHCO NMe Z-4                                                         1-2148 5 NHCO NMe Z-5                                                         1-2149 5 NHCO NMe Z-6                                                         1-2150 5 NHCO NMe Z-7                                                         1-2151 5 NHCO NMe Z-8                                                         1-2152 5 NHCO NMe Z-9                                                         1-2153 5 NHCO NMe Z-10                                                        1-2154 5 NHCO NMe Z-11                                                        1-2155 5 NHCO NMe Z-12                                                        1-2156 5 NHCO NMe 3-Py                                                        1-2157 5 NHCO NMe 4-Py                                                        1-2158 5 NHCO NHNH H                                                          1-2159 5 NHCO NHNH Me                                                         1-2160 5 NHCO NHNH Et                                                         1-2161 5 NHCO NHNMe Me                                                        1-2162 5 NHCO NHNMe Et                                                        1-2163 5 NHCO NHNMe Pr                                                        1-2164 5 NHCONHNHCO NH H                                                      1-2165 5 NHCONHNHCO NH Ph                                                     1-2166 5 NHCONHNHCO NH 2-Me--Ph                                               1-2167 5 NHCONHNHCO NH 4-Me--Ph                                               1-2168 5 NHCONHNHCO NH 2,4-diMe--Ph                                           1-2169 5 NHCONHNHCO NH 3,4-diMe--Ph                                           1-2170 5 NHCONHNHCO NH 2-(CF.sub.3)Ph                                         1-2171 5 NHCONHNHCO NH 4-(CF.sub.3)Ph                                         1-2172 5 NHCONHNHCO NH 2-MeOPh                                                1-2173 5 NHCONHNHCO NH 4-MeOPh                                                1-2174 5 NHCONHNHCO NH 2-EtOPh                                                1-2175 5 NHCONHNHCO NH 4-EtOPh                                                1-2176 5 NHCONHNHCO NH 2-HOPh                                                 1-2177 5 NHCONHNHCO NH 4-HOPh                                                 1-2178 5 NHCONHNHCO NH 2-(HOOC)Ph                                             1-2179 5 NHCONHNHCO NH 4-(HOOC)Ph                                             1-2180 5 NHCONHNHCO NH 2-(MeOOC)Ph                                            1-2181 5 NHCONHNHCO NH 4-(MeOOC)Ph                                            1-2182 5 NHCONHNHCO NH 2-(EtOOC)Ph                                            1-2183 5 NHCONHNHCO NH 4-(EtOOC)Ph                                            1-2184 5 NHCONHNHCO NH 2-(tBuOOC)Ph                                           1-2185 5 NHCONHNHCO NH 4-(tBuOOC)Ph                                           1-2186 5 NHCONHNHCO NH 2-Cl--Ph                                               1-2187 5 NHCONHNHCO NH 4-Cl--Ph                                               1-2188 5 NHCONHNHCO NH 2-Br--Ph                                               1-2189 5 NHCONHNHCO NH 4-Br--Ph                                               1-2190 5 NHCONHNHCO NH 2-I--Ph                                                1-2191 5 NHCONHNHCO NH 4-I--Ph                                                1-2192 5 NHCONHNHCO NH 2-NO.sub.2 --Ph                                        1-2193 5 NHCONHNHCO NH 4-NO.sub.2 --Ph                                        1-2194 5 NHCONHNHCO NH 2-NH.sub.2 --Ph                                        1-2195 5 NHCONHNHCO NH 4-NH.sub.2 --Ph                                        1-2196 5 NHCONHNHCO NH 2-(HO.sub.3 S)Ph                                       1-2197 5 NHCONHNHCO NH 4-(HO.sub.3 S)Ph                                       1-2198 5 NHCONHNHCO NH 2-(NH.sub.2 O.sub.2 S)Ph                               1-2199 5 NHCONHNHCO NH 4-(NH.sub.2 O.sub.2 S)Ph                               1-2200 5 NHCONHNHCO NH 2-CN--Ph                                               1-2201 5 NHCONHNHCO NH 4-CN--Ph                                               1-2202 5 NHCONHNHCO NH 2-(HOCH.sub.2)Ph                                       1-2203 5 NHCONHNHCO NH 4-(HOCH.sub.2)Ph                                       1-2204 5 NHCONHNHCO NH Me                                                     1-2205 5 NHCONHNHCO NH Et                                                     1-2206 5 NHCONHNHCO NH Pr                                                     1-2207 5 NHCONHNHCO NH iPr                                                    1-2208 5 NHCONHNHCO NH Bu                                                     1-2209 5 NHCONHNHCO NH HOOCCH.sub.2 --                                        1-2210 5 NHCONHNHCO NH MeOOCCH.sub.2 --                                       1-2211 5 NHCONHNHCO NH MeCH(COOH)                                             1-2212 5 NHCONHNHCO NH HOOC--(CH.sub.2).sub.2 --                              1-2213 5 NHCONHNHCO NH MeCH(COOMe)                                            1-2214 5 NHCONHNHCO NH 1-HOOC-iBu                                             1-2215 5 NHCONHNHCO NH 1-MeOOC-iBu                                            1-2216 5 NHCONHNHCO NH 1-HOOC-iPn                                             1-2217 5 NHCONHNHCO NH 1-MeOOC-iPn                                            1-2218 5 NHCONHNHCO NH 1-HOOC-2-Me--Bu                                        1-2219 5 NHCONHNHCO NH 1-MeOOC-2-Me--Bu                                       1-2220 5 NHCONHNHCO NH CH.sub.2 CH.sub.2 SO.sub.3 H                           1-2221 5 NHCONHNHCO NH OH                                                     1-2222 5 NHCONHNHCO NH MeO                                                    1-2223 5 NHCONHNHCO NH EtO                                                    1-2224 5 NHCONHNHCO NH PrO                                                    1-2225 5 NHCONHNHCO NH iPrO                                                   1-2226 5 NHCONHNHCO NH BuO                                                    1-2227 5 NHCONHNHCO NH iBuO                                                   1-2228 5 NHCONHNHCO NH sBuO                                                   1-2229 5 NHCONHNHCO NH tBuO                                                   1-2230 5 NHCONHNHCO NH HxO                                                    1-2231 5 NHCONHNHCO NH PhO                                                    1-2232 5 NHCONHNHCO NH BzO                                                    1-2233 5 NHCONHNHCO NH Z-1                                                    1-2234 5 NHCONHNHCO NH Z-2                                                    1-2235 5 NHCONHNHCO NH Z-3                                                    1-2236 5 NHCONHNHCO NH Z-4                                                    1-2237 5 NHCONHNHCO NH Z-5                                                    1-2238 5 NHCONHNHCO NH Z-6                                                    1-2239 5 NHCONHNHCO NH Z-7                                                    1-2240 5 NHCONHNHCO NH Z-8                                                    1-2241 5 NHCONHNHCO NH Z-9                                                    1-2242 5 NHCONHNHCO NH Z-10                                                   1-2243 5 NHCONHNHCO NH Z-11                                                   1-2244 5 NHCONHNHCO NH Z-12                                                   1-2245 5 NHCONHNHCO NH 3-Py                                                   1-2246 5 NHCONHNHCO NH 4-Py                                                   1-2247 5 NHCONHCO -- H                                                        1-2248 5 NHCONHCO -- Ph                                                       1-2249 5 NHCONHCO -- 2-Me--Ph                                                 1-2250 5 NHCONHCO -- 4-Me--Ph                                                 1-2251 5 NHCONHCO -- 2,4-diMe--Ph                                             1-2252 5 NHCONHCO -- 3,4-diMe--Ph                                             1-2253 5 NHCONHCO -- 2-(CF.sub.3)Ph                                           1-2254 5 NHCONHCO -- 4-(CF.sub.3)Ph                                           1-2255 5 NHCONHCO -- 2-MeOPh                                                  1-2256 5 NHCONHCO -- 4-MeOPh                                                  1-2257 5 NHCONHCO -- 2-EtOPh                                                  1-2258 5 NHCONHCO -- 4-EtOPh                                                  1-2259 5 NHCONHCO -- 2-HOPh                                                   1-2260 5 NHCONHCO -- 4-HOPh                                                   1-2261 5 NHCONHCO -- 2-(HOOC)Ph                                               1-2262 5 NHCONHCO -- 4-(HOOC)Ph                                               1-2263 5 NHCONHCO -- 2-(MeOOC)Ph                                              1-2264 5 NHCONHCO -- 4-(MeOOC)Ph                                              1-2265 5 NHCONHCO -- 2-(EtOOC)Ph                                              1-2266 5 NHCONHCO -- 4-(EtOOC)Ph                                              1-2267 5 NHCONHCO -- 2-(tBuOOC)Ph                                             1-2268 5 NHCONHCO -- 4-(tBuOOC)Ph                                             1-2269 5 NHCONHCO -- 2-Cl--Ph                                                 1-2270 5 NHCONHCO -- 4-Cl--Ph                                                 1-2271 5 NHCONHCO -- 2-Br--Ph                                                 1-2272 5 NHCONHCO -- 4-Br--Ph                                                 1-2273 5 NHCONHCO -- 2-I--Ph                                                  1-2274 5 NHCONHCO -- 4-I--Ph                                                  1-2275 5 NHCONHCO -- 2-NO.sub.2 --Ph                                          1-2276 5 NHCONHCO -- 4-NO.sub.2 --Ph                                          1-2277 5 NHCONHCO -- 2-NH.sub.2 --Ph                                          1-2278 5 NHCONHCO -- 4-NH.sub.2 --Ph                                          1-2279 5 NHCONHCO -- 2-(HO.sub.3 S)Ph                                         1-2280 5 NHCONHCO -- 4-(HO.sub.3 S)Ph                                         1-2281 5 NHCONHCO -- 2-(NH.sub.2 O.sub.2 S)Ph                                 1-2282 5 NHCONHCO -- 4-(NH.sub.2 O.sub.2 S)Ph                                 1-2283 5 NHCONHCO -- 2-CN--Ph                                                 1-2284 5 NHCONHCO -- 4-CN--Ph                                                 1-2285 5 NHCONHCO -- 2-(HOCH.sub.2)Ph                                         1-2286 5 NHCONHCO -- 4-(HOCH.sub.2)Ph                                         1-2287 5 NHCONHCO -- Me                                                       1-2288 5 NHCONHCO -- Et                                                       1-2289 5 NHCONHCO -- Pr                                                       1-2290 5 NHCONHCO -- iPr                                                      1-2291 5 NHCONHCO -- Bu                                                       1-2292 5 NHCONHCO -- HOOCCH.sub.2 --                                          1-2293 5 NHCONHCO -- MeOOCCH.sub.2 --                                         1-2294 5 NHCONHCO -- MeCH(COOH)                                               1-2295 5 NHCONHCO -- HOOC--(CH.sub.2).sub.2 --                                1-2296 5 NHCONHCO -- MeCH(COOMe)                                              1-2297 5 NHCONHCO -- 1-HOOC-iBu                                               1-2298 5 NHCONHCO -- 1-MeOOC-iBu                                              1-2299 5 NHCONHCO -- 1-HOOC-iPn                                               1-2300 5 NHCONHCO -- 1-MeOOC-iPn                                              1-2301 5 NHCONHCO -- 1-HOOC-2-Me--Bu                                          1-2302 5 NHCONHCO -- 1-MeOOC-2-Me--Bu                                         1-2303 5 NHCONHCO -- CH.sub.2 CH.sub.2 SO.sub.3 H                             1-2304 5 NHCONHCO -- MeO                                                      1-2305 5 NHCONHCO -- EtO                                                      1-2306 5 NHCONHCO -- PrO                                                      1-2307 5 NHCONHCO -- iPrO                                                     1-2308 5 NHCONHCO -- BuO                                                      1-2309 5 NHCONHCO -- iBuO                                                     1-2310 5 NHCONHCO -- sBuO                                                     1-2311 5 NHCONHCO -- tBuO                                                     1-2312 5 NHCONHCO -- HxO                                                      1-2313 5 NHCONHCO -- PhO                                                      1-2314 5 NHCONHCO -- BzO                                                      1-2315 5 NHCONHCO -- Z-1                                                      1-2316 5 NHCONHCO -- Z-2                                                      1-2317 5 NHCONHCO -- Z-3                                                      1-2318 5 NHCONHCO -- Z-4                                                      1-2319 5 NHCONHCO -- Z-5                                                      1-2320 5 NHCONHCO -- Z-6                                                      1-2321 5 NHCONHCO -- Z-7                                                      1-2322 5 NHCONHCO -- Z-8                                                      1-2323 5 NHCONHCO -- Z-9                                                      1-2324 5 NHCONHCO -- Z-10                                                     1-2325 5 NHCONHCO -- Z-11                                                     1-2326 5 NHCONHCO -- Z-12                                                     1-2327 5 NHCONHCO -- 3-Py                                                     1-2328 5 NHCONHCO -- 4-Py                                                     1-2329 5 NHCONHSO.sub.2 -- H                                                  1-2330 5 NHCONHSO.sub.2 -- Ph                                                 1-2331 5 NHCONHSO.sub.2 -- 2-Me--Ph                                           1-2332 5 NHCONHSO.sub.2 -- 4-Me--Ph                                           1-2333 5 NHCONHSO.sub.2 -- 2,4-diMe--Ph                                       1-2334 5 NHCONHSO.sub.2 -- 3,4-diMe--Ph                                       1-2335 5 NHCONHSO.sub.2 -- 2-(CF.sub.3)Ph                                     1-2336 5 NHCONHSO.sub.2 -- 4-(CF.sub.3)Ph                                     1-2337 5 NHCONHSO.sub.2 -- 2-MeOPh                                            1-2338 5 NHCONHSO.sub.2 -- 4-MeOPh                                            1-2339 5 NHCONHSO.sub.2 -- 2-EtOPh                                            1-2340 5 NHCONHSO.sub.2 -- 4-EtOPh                                            1-2341 5 NHCONHSO.sub.2 -- 2-HOPh                                             1-2342 5 NHCONHSO.sub.2 -- 4-HOPh                                             1-2343 5 NHCONHSO.sub.2 -- 2-(HOOC)Ph                                         1-2344 5 NHCONHSO.sub.2 -- 4-(HOOC)Ph                                         1-2345 5 NHCONHSO.sub.2 -- 2-(MeOOC)Ph                                        1-2346 5 NHCONHSO.sub.2 -- 4-(MeOOC)Ph                                        1-2347 5 NHCONHSO.sub.2 -- 2-(EtOOC)Ph                                        1-2348 5 NHCONHSO.sub.2 -- 4-(EtOOC)Ph                                        1-2349 5 NHCONHSO.sub.2 -- 2-(tBuOOC)Ph                                       1-2350 5 NHCONHSO.sub.2 -- 4-(tBuOOC)Ph                                       1-2351 5 NHCONHSO.sub.2 -- 2-Cl--Ph                                           1-2352 5 NHCONHSO.sub.2 -- 4-Cl--Ph                                           1-2353 5 NHCONHSO.sub.2 -- 2-Br--Ph                                           1-2354 5 NHCONHSO.sub.2 -- 4-Br--Ph                                           1-2355 5 NHCONHSO.sub.2 -- 2-I--Ph                                            1-2356 5 NHCONHSO.sub.2 -- 4-I--Ph                                            1-2357 5 NHCONHSO.sub.2 -- 2-NO.sub.2 --Ph                                    1-2358 5 NHCONHSO.sub.2 -- 4-NO.sub.2 --Ph                                    1-2359 5 NHCONHSO.sub.2 -- 2-NH.sub.2 --Ph                                    1-2360 5 NHCONHSO.sub.2 -- 4-NH.sub.2 --Ph                                    1-2361 5 NHCONHSO.sub.2 -- 2-(HO.sub.3 S)Ph                                   1-2362 5 NHCONHSO.sub.2 -- 4-(HO.sub.3 S)Ph                                   1-2363 5 NHCONHSO.sub.2 -- 2-(NH.sub.2 O.sub.2 S)Ph                           1-2364 5 NHCONHSO.sub.2 -- 4-(NH.sub.2 O.sub.2 S)Ph                           1-2365 5 NHCONHSO.sub.2 -- 2-CN--Ph                                           1-2366 5 NHCONHSO.sub.2 -- 4-CN--Ph                                           1-2367 5 NHCONHSO.sub.2 -- 2-(HOCH.sub.2)Ph                                   1-2368 5 NHCONHSO.sub.2 -- 4-(HOCH.sub.2)Ph                                   1-2369 5 NHCONHSO.sub.2 -- Me                                                 1-2370 5 NHCONHSO.sub.2 -- Et                                                 1-2371 5 NHCONHSO.sub.2 -- Pr                                                 1-2372 5 NHCONHSO.sub.2 -- iPr                                                1-2373 5 NHCONHSO.sub.2 -- Bu                                                 1-2374 5 NHCONHSO.sub.2 -- HOOCCH.sub.2                                       1-2375 5 NHCONHSO.sub.2 -- MeOOCCH.sub.2                                      1-2376 5 NHCONHSO.sub.2 -- MeCH(COOH)                                         1-2377 5 NHCONHSO.sub.2 -- HOOC--(CH.sub.2).sub.2                             1-2378 5 NHCONHSO.sub.2 -- MeCH(COOMe)                                        1-2379 5 NHCONHSO.sub.2 -- 1-HOOC-iBu                                         1-2380 5 NHCONHSO.sub.2 -- 1-MeOOC-iBu                                        1-2381 5 NHCONHSO.sub.2 -- 1-HOOC-iPn                                         1-2382 5 NHCONHSO.sub.2 -- 1-MeOOC-iPn                                        1-2383 5 NHCONHSO.sub.2 -- 1-HOOC-2-Me--Bu                                    1-2384 5 NHCONHSO.sub.2 -- 1-MeOOC-2-Me--Bu                                   1-2385 5 NHCONHSO.sub.2 -- CH.sub.2 CH.sub.2 SO.sub.3 H                       1-2386 5 NHCONHSO.sub.2 -- OH                                                 1-2387 5 NHCONHSO.sub.2 -- MeO                                                1-2388 5 NHCONHSO.sub.2 -- EtO                                                1-2389 5 NHCONHSO.sub.2 -- PrO                                                1-2390 5 NHCONHSO.sub.2 -- iPrO                                               1-2391 5 NHCONHSO.sub.2 -- BuO                                                1-2392 5 NHCONHSO.sub.2 -- iBuO                                               1-2393 5 NHCONHSO.sub.2 -- sBuO                                               1-2394 5 NHCONHSO.sub.2 -- tBuO                                               1-2395 5 NHCONHSO.sub.2 -- HxO                                                1-2396 5 NHCONHSO.sub.2 -- PhO                                                1-2397 5 NHCONHSO.sub.2 -- BzO                                                1-2398 5 NHCONHSO.sub.2 -- Z-1                                                1-2399 5 NHCONHSO.sub.2 -- Z-2                                                1-2400 5 NHCONHSO.sub.2 -- Z-3                                                1-2401 5 NHCONHSO.sub.2 -- Z-4                                                1-2402 5 NHCONHSO.sub.2 -- Z-5                                                1-2403 5 NHCONHSO.sub.2 -- Z-6                                                1-2404 5 NHCONHSO.sub.2 -- Z-7                                                1-2405 5 NHCONHSO.sub.2 -- Z-8                                                1-2406 5 NHCONHSO.sub.2 -- Z-9                                                1-2407 5 NHCONHSO.sub.2 -- Z-10                                               1-2408 5 NHCONHSO.sub.2 -- Z-11                                               1-2409 5 NHCONHSO.sub.2 -- Z-12                                               1-2410 5 NHCONHSO.sub.2 -- 3-Py                                               1-2411 5 NHCONHSO.sub.2 -- 4-Py                                               1-2412 5 NHCONHSO.sub.2 NH H                                                  1-2413 5 NHCONHSO.sub.2 NH Me                                                 1-2414 5 NHCONHSO.sub.2 NH Et                                                 1-2415 5 NHCONHSO.sub.2 NH Pr                                                 1-2416 5 NHCONHSO.sub.2 NH iPr                                                1-2417 5 NHCONHSO.sub.2 NH Bu                                                 1-2418 5 NHCONHSO.sub.2 NMe Me                                                1-2419 5 NHCONHSO.sub.2 NMe Et                                                1-2420 5 NHCONHSO.sub.2 NMe Pr                                                1-2421 5 NHCONHSO.sub.2 NMe iPr                                               1-2422 5 NHCONHSO.sub.2 NMe Bu                                                1-2423 5 -- NH H                                                              1-2424 5 -- NH Me                                                             1-2425 5 -- NH Et                                                             1-2426 5 -- NH Pr                                                             1-2427 5 -- NH iPr                                                            1-2428 5 -- NH Bu                                                           1-2429                                                                            5   CO         Pyr                                                          1-2430 5 CO Pipri                                                             1-2431 5 CO Pipra                                                             1-2432 5 CO Mor                                                               1-2433 5 CO Thmor                                                             1-2434 5 CO NHPyr                                                             1-2435 5 CO NHPipri                                                           1-2436 5 CO NHPipra                                                           1-2437 5 CO NHMor                                                             1-2438 5 CO NHThmor                                                           1-2439 5 NHCO Pyr                                                             1-2440 5 NHCO Pipri                                                           1-2441 5 NHCO Pipra                                                           1-2442 5 NHCO Mor                                                             1-2443 5 NHCO Thmor                                                           1-2444 5 NHCO NHPyr                                                           1-2445 5 NHCO NHPipri                                                         1-2446 5 NHCO NHPipra                                                         1-2447 5 NHCO NHMor                                                           1-2448 5 NHCO NHThmor                                                         1-2449 5 CONHCO Pyr                                                           1-2450 5 CONHCO Pipri                                                         1-2451 5 CONHCO Pipra                                                         1-2452 5 CONHCO Mor                                                           1-2453 5 CONHCO Thmor                                                         1-2454 5 CONHCO NHPyr                                                         1-2455 5 CONHCO NHPipri                                                       1-2456 5 CONHCO NHPipra                                                       1-2457 5 CONHCO NHMor                                                         1-2458 5 CONHCO NHThmor                                                       1-2459 5 CONHSO.sub.2 Pyr                                                     1-2460 5 CONHSO.sub.2 Pipri                                                   1-2461 5 CONHSO.sub.2 Pipra                                                   1-2462 5 CONHSO.sub.2 Mor                                                     1-2463 5 CONHSO.sub.2 Thmor                                                   1-2464 5 CONHSO.sub.2 NHPyr                                                   1-2465 5 CONHSO.sub.2 NHPipri                                                 1-2466 5 CONHSO.sub.2 NHPipra                                                 1-2467 5 CONHSO.sub.2 NHMor                                                   1-2468 5 CONHSO.sub.2 NHThmor                                               1-2469                                                                            5   NHSO.sub.2 NH     Z-4                                                   1-2470 5 NHSO.sub.2 -- Me                                                     1-2471 5 NHSO.sub.2 -- Et                                                     1-2472 5 NHSO.sub.2 -- Pr                                                     1-2473 5 NHSO.sub.2 -- CH.sub.2 Cl                                            1-2474 5 NHSO.sub.2 -- Ph                                                     1-2475 5 NHSO.sub.2 -- 4-Me--Ph                                               1-2476 5 CO NMe Ph                                                            1-2477 5 CO NMe 2-Me--PH                                                      1-2478 5 CO NMe 4-Me--Ph                                                      1-2479 5 CO NMe 2,4-diMe--Ph                                                  1-2480 5 CO NMe 3,4-diMe--Ph                                                  1-2481 5 CO NMe 2-(CF.sub.3)Ph                                                1-2482 5 CO NMe 4-(CF.sub.3)Ph                                                1-2483 5 CO NMe 2-MeOPh                                                       1-2484 5 CO NMe 4-MeOPh                                                       1-2485 5 CO NMe 2-EtOPh                                                       1-2486 5 CO NMe 4-EtOPh                                                       1-2487 5 CO NMe 2-HOPh                                                        1-2488 5 CO NMe 4-HOPh                                                        1-2489 5 CO NMe 2-(HOOC)Ph                                                    1-2490 5 CO NMe 4-(HOOC)Ph                                                    1-2491 5 CO NMe 2-(MeOOC)Ph                                                   1-2492 5 CO NMe 4-(MeOOC)Ph                                                   1-2493 5 CO NMe 2-(EtOOC)Ph                                                   1-2494 5 CO NMe 4-(EtOOC)Ph                                                   1-2495 5 CO NMe 2-(tBuOOC)Ph                                                  1-2496 5 CO NMe 4-(tBuOOC)Ph                                                  1-2497 5 CO NMe 2-Cl--Ph                                                      1-2498 5 CO NMe 4-Cl--Ph                                                      1-2499 5 CO NMe 2-Br--Ph                                                      1-2500 5 CO NMe 4-Br--Ph                                                      1-2501 5 CO NMe 2-I--Ph                                                       1-2502 5 CO NMe 4-I--Ph                                                       1-2503 5 CO NMe 2-NO.sub.2 --Ph                                               1-2504 5 CO NMe 4-NO.sub.2 --Ph                                               1-2505 5 CO NMe 2-NH.sub.2 --Ph                                               1-2506 5 CO NMe 4-NH.sub.2 --Ph                                               1-2507 5 CO NMe 2-(HO.sub.3 S)Ph                                              1-2508 5 CO NMe 4-(HO.sub.3 S)Ph                                              1-2509 5 CO NMe 2-(NH.sub.2 O.sub.2 S)Ph                                      1-2510 5 CO NMe 4-(NH.sub.2 O.sub.2 S)Ph                                      1-2511 5 CO NMe 2-CN--Ph                                                      1-2512 5 CO NMe 4-CN--Ph                                                      1-2513 5 CO NMe 2-(HOCH.sub.2)Ph                                              1-2514 5 CO NMe 4-(HOCH.sub.2)Ph                                              1-2515 5 CO NMe Me                                                            1-2516 5 CO NMe Et                                                            1-2517 5 CO NMe Pr                                                            1-2518 5 CO NMe iPr                                                           1-2519 5 CO NMe Bu                                                            1-2520 5 CO NMe HOOCCH.sub.2                                                  1-2521 5 CO NMe HOOC--(CH.sub.2).sub.2                                        1-2522 5 CO NMe MeCH(COOH)                                                    1-2523 5 CO NMe HOOC--(CH.sub.2).sub.3 --                                     1-2524 5 CO NMe MeCH(COOMe)                                                   1-2525 5 CO NMe 1-HOOC-iBu                                                    1-2526 5 CO NMe 1-MeOOC-iBu                                                   1-2527 5 CO NMe 1-HOOC-iPn                                                    1-2528 5 CO NMe 1-MeOCC-iPn - 1-2529 5 CO NMe 1-HOOC-2-Me--Bu                 1-2530 5 CO NMe 1-MeOOC-2-Me--Bu                                              1-2531 5 CO NMe CH.sub.2 CH.sub.2 SO.sub.3 H                                  1-2532 5 CO NMe OH                                                            1-2533 5 CO NMe MeO                                                           1-2534 5 CO NMe EtO                                                           1-2535 5 CO NMe PrO                                                           1-2536 5 CO NMe iPrO                                                          1-2537 5 CO NMe BuO                                                           1-2538 5 CO NMe iBuO                                                          1-2539 5 CO NMe sBuO                                                          1-2540 5 CO NMe tBuO                                                          1-2541 5 CO NMe HxO                                                           1-2542 5 CO NMe PhO                                                           1-2543 5 CO NMe BzO                                                           1-2544 5 CO NMe Z-1                                                           1-2545 5 CO NMe Z-2                                                           1-2546 5 CO NMe Z-3                                                           1-2547 5 CO NMe Z-4                                                           1-2548 5 CO NMe Z-5                                                           1-2549 5 CO NMe Z-6                                                           1-2550 5 CO NMe Z-7                                                           1-2551 5 CO NMe Z-8                                                           1-2552 5 CO NMe Z-9                                                           1-2553 5 CO NMe Z-10                                                          1-2554 5 CO NMe Z-11                                                          1-2555 5 CO NMe Z-12                                                          1-2556 5 CO NMe 3-Py                                                          1-2557 5 CO NMe 4-Py                                                        1-2558                                                                            5   CO         Thiad                                                        1-2559 5 CO NHThiad                                                           1-2560 5 NHCO Thiad                                                           1-2561 5 NHCO NHThiad                                                         1-2562 5 CONHCO Thiad                                                         1-2563 5 CONHCO NHThiad                                                       1-2564 5 CONHSO.sub.2 Thiad                                                   1-2565 5 CONHSO.sub.2 NHThiad                                               1-2566                                                                            5   NHCS       NH     H                                                     1-2567 5 NHCS NH Me                                                           1-2568 5 NHCS NH Et                                                           1-2569 5 NHCS NH Ph                                                           1-2570 5 NHCS NH HOOCCH.sub.2                                                 1-2571 5 NHCS NH MeOOCCH.sub.2                                                1-2572 5 NHCS NH MeCH(COOH)                                                   1-2573 5 NHCS NH HOOC--(CH.sub.2).sub.2                                       1-2574 5 NHCS NH MeCH(COOMe)                                                  1-2575 5 CO NH HOOC--(CH.sub.2).sub.3 --                                      1-2576 5 NHCO NH HOOC--(CH.sub.2).sub.3 --                                    1-2577 5 NHCO -- HOOC--(CH.sub.2).sub.3 --                                    1-2578 5 NHCS NH HOOC--(CH.sub.2).sub.3 --                                    1-2579 5 CO NH MeSO.sub.2 NHCOCH(Me)                                          1-2580 5 NHCO NH MeSO.sub.2 NHCOCH(Me)                                        1-2581 5 NHCO -- MeSO.sub.2 NHCOCH(Me)                                        1-2582 5 NHCS NH MeSO.sub.2 NHCOCH(Me)                                        1-2583 5 -- NH HOOCCH.sub.2                                                   1-2584 5 -- NH MeOOCCH.sub.2                                                  1-2585 5 -- NH MeCH(COOH)                                                     1-2586 5 -- NH HOOC--(CH.sub.2).sub.2                                         1-2587 5 -- NH MeCH(COOMe)                                                    1-2588 5 -- NH HOOC--(CH.sub.2).sub.3 --                                      1-2589 5 NHCOCO -- OH                                                         1-2590 5 NHCOCO -- MeO                                                        1-2591 5 NHCOCO -- EtO                                                        1-2592 5 NHCOCO -- PrO                                                        1-2593 5 NHCOCO -- iPrO                                                       1-2594 5 NHCOCO -- BuO                                                        1-2595 5 NHCOCO -- iBuO                                                       1-2596 5 NHCOCO -- sBuO                                                       1-2597 5 NHCOCO -- tBuO                                                       1-2598 5 NHCOCO -- HxO                                                        1-2599 5 NHCOCO -- PhO                                                        1-2600 5 NHCOCO -- BzO                                                      1-2601                                                                            0   --         1,3-diox-IInd                                                1-2602 1 -- 1,3-diox-IInd                                                     1-2603 2 -- 1,3-diox-IInd                                                     1-2604 3 -- 1,3-diox-IInd                                                     1-2605 4 -- 1,3-diox-IInd                                                     1-2606 5 -- 1,3-diox-IInd                                                     1-2607 6 -- 1,3-diox-IInd                                                     1-2608 7 -- 1,3-diox-IInd                                                     1-2609 8 -- 1,3-diox-IInd                                                     1-2610 9 -- 1,3-diox-IInd                                                     1-2611 10 -- 1,3-diox-IInd                                                    1-2612 11 -- 1,3-diox-IInd                                                    1-2613 12 -- 1,3-diox-IInd                                                  1-2614                                                                            4   NHCONHSO.sub.2 NHCO                                                                      NH     Z-4                                                   1-2615 4 NHCONHSO.sub.2 NHCO NH Pn                                            1-2616 2 O -- H                                                               1-2617 4 O -- H                                                               1-2618 5 O -- H                                                               1-2619 5 O -- Ph                                                              1-2620 5 O -- 2-Py                                                            1-2621 5 O -- 3-Py                                                            1-2622 5 O -- 4-Py                                                            1-2623 5 O -- Z-1                                                             1-2624 5 O -- Z-2                                                             1-2625 5 O -- Z-3                                                             1-2626 5 O -- Z-4                                                             1-2627 5 O -- Z-5                                                             1-2628 5 O -- Z-6                                                             1-2629 5 O -- Z-7                                                             1-2630 5 O -- Z-8                                                             1-2631 5 O -- Z-9                                                             1-2632 5 O -- Z-10                                                            1-2633 5 O -- Z-11                                                            1-2634 5 O -- Z-12                                                            1-2635 4 NHCO -- 3-Py                                                         1-2636 5 NHCO -- 3-Py                                                         1-2637 4 CO NH HOCH.sub.2 CH(CH.sub.3)CH.sub.2                                1-2638 5 CO NH HOCH.sub.2 CH(CH.sub.3)CH.sub.2                                1-2639 4 NHCO NH HOCH.sub.2 CH(CH.sub.3)CH.sub.2                              1-2640 5 NHCO NH HOCH.sub.2 CH(CH.sub.3)CH.sub.2                              1-2641 4 CO NH MeSO.sub.2 NHCOCH.sub.2                                        1-2642 5 CO NH MeSO.sub.2 NHCOCH.sub.2                                        1-2643 4 NHCO NH MeSO.sub.2 NHCOCH.sub.2                                      1-2644 5 NHCO NH MeSO.sub.2 NHCOCH.sub.2                                      1-2645 4 CO NH H.sub.2 NSO.sub.2 NHCOCH.sub.2                                 1-2646 5 CO NH H.sub.2 NSO.sub.2 NHCOCH.sub.2                                 1-2647 4 NHCO NH H.sub.2 NSO.sub.2 NHCOCH.sub.2                               1-2648 5 NHCO NH H.sub.2 NSO.sub.2 NHCOCH.sub.2                               1-2649 4 CO NH 1-(MeSO.sub.2 NHCO)--Et                                        1-2650 5 CO NH 1-(MeSO.sub.2 NHCO)--Et                                        1-2651 4 NHCO NH 1-(MeSO.sub.2 NHCO)--Et                                      1-2652 5 NHCO NH 1-(MeSO.sub.2 NHCO)--Et                                      1-2653 4 CO NH 1-(H.sub.2 NSO.sub.2 NHCO)--Et                                 1-2654 5 CO NH 1-(H.sub.2 NSO.sub.2 NHCO)--Et                                 1-2655 4 NHCO NH 1-(H.sub.2 NSO.sub.2 NHCO)--Et                               1-2656 5 NHCO NH 1-(H.sub.2 NSO.sub.2 NHCO)--Et                               1-2657 4 CO NH HOOC--(CH.sub.2).sub.4                                         1-2658 5 CO NH HOOC--(CH.sub.2).sub.4                                         1-2659 4 NHCO NH HOOC--(CH.sub.2).sub.4                                       1-2660 5 NHCO NH HOOC--(CH.sub.2).sub.4                                       1-2661 4 CO NH HO--(CH.sub.2).sub.2                                           1-2662 5 CO NH HO--(CH.sub.2).sub.2                                           1-2663 4 NHCO NH HO--(CH.sub.2).sub.2                                         1-2664 5 NHCO NH HO--(CH.sub.2).sub.2                                         1-2665 4 CO NH HO--CH.sub.2 --CH(CH.sub.3)                                    1-2666 5 CO NH HO--CH.sub.2 --CH(CH.sub.3)                                    1-2667 4 NHCO NH HO--CH.sub.2 --CH(CH.sub.3)                                  1-2668 5 NHCO NH HO--CH.sub.2 --CH(CH.sub.3)                                  1-2669 4 CO NMe HOOC--(CH.sub.2).sub.3                                        1-2670 4 NHCO NMe HOOC--(CH.sub.2).sub.3                                      1-2671 5 NHCO NMe HOOC--(CH.sub.2).sub.3                                      1-2672 4 CONMeSO.sub.2 -- Me                                                  1-2673 5 CONMeSO.sub.2 -- Me                                                1-2674                                                                            4   CO         1-Indn                                                       1-2675 5 CO 1-Indn                                                            1-2676 4 NHCO 1-Indn                                                          1-2677 5 NHCO 1-Indn                                                          1-2678 4 CO 2-(HOOC)-1-Indn                                                   1-2679 5 CO 2-(HOOC)-1-Indn                                                   1-2680 4 NHCO 2-(HOOC)-1-Indn                                                 1-2681 5 NHCO 2-(HOOC)-1-Indn                                                 1-2682 4 -- 3,4-diMe-2,5-diox-1-Imdd                                          1-2683 5 -- 3,4-diMe-2,5-diox-1-Imdd                                        1-2684                                                                            4   CONHSO.sub.2                                                                             --     CF.sub.3                                            __________________________________________________________________________     ##STR6##

                  TABLE 2                                                         ______________________________________                                        Cpd.                                                                            No.     k     A           B     R.sup.1                                     ______________________________________                                        2-1   4     CO            NH    H                                               2-2 4 CO NH Ph                                                                2-3 4 CO NH 2-Me-Ph                                                           2-4 4 CO NH 4-Me-Ph                                                           2-5 4 CO NH 2,4-diMe-Ph                                                       2-6 4 CO NH 3,4-diMe-Ph                                                       2-7 4 CO NH 2-(CF.sub.3)-Ph                                                   2-8 4 CO NH 4-(CF.sub.3)-Ph                                                   2-9 4 CO NH 2-MeOPh                                                           2-10 4 CO NH 4-MeOPh                                                          2-11 4 CO NH 2-EtOPh                                                          2-12 4 CO NH 4-EtOPh                                                          2-13 4 CO NH 2-HOPh                                                           2-14 4 CO NH 4-HOPh                                                           2-15 4 CO NH 2-(HOOC)-Ph                                                      2-16 4 CO NH 4-(HOOC)-Ph                                                      2-17 4 CO NH 2-(MeOOC)-Ph                                                     2-18 4 CO NH 4-(MeOOC)-Ph                                                     2-19 4 CO NH 2-(EtOOC)-Ph                                                     2-20 4 CO NH 4-(EtOOC)-Ph                                                     2-21 4 CO NH 2-(tBuOOC)-Ph                                                    2-22 4 CO NH 4-(tBuOOC)-Ph                                                    2-23 4 CO NH 2-Cl-Ph                                                          2-24 4 CO NH 4-Cl-Ph                                                          2-25 4 CO NH 2-Br-Ph                                                          2-26 4 CO NH 4-Br-Ph                                                          2-27 4 CO NH 2-I-Ph                                                           2-28 4 CO NH 4-I-Ph                                                           2-29 4 CO NH 2-NO.sub.2 -Ph                                                   2-30 4 CO NH 4-NO.sub.2 -Ph                                                   2-31 4 CO NH 2-NH.sub.2 -Ph                                                   2-32 4 CO NH 4-NH.sub.2 -Ph                                                   2-33 4 CO NH 2-(HO.sub.3 S)-Ph                                                2-34 4 CO NH 4-(HO.sub.3 S)-Ph                                                2-35 4 CO NH 2-NH.sub.2 O.sub.2 S)-Ph                                         2-36 4 CO NH 4-(NH.sub.2 O.sub.2 S)-Ph                                        2-37 4 CO NH 2-CN-Ph                                                          2-38 4 CO NH 4-CN-Ph                                                          2-39 4 CO NH 2-(HOCH.sub.2)-Ph                                                2-40 4 CO NH 4-(HOCH.sub.2)-Ph                                                2-41 4 CO NH Me                                                               2-42 4 CO NH Et                                                               2-43 4 CO NH Pr                                                               2-44 4 CO NH iPr                                                              2-45 4 CO NH Bu                                                               2-46 4 CO NH HOOCCH.sub.2 --                                                  2-47 4 CO NH MeOOCCH.sub.2 --                                                 2-48 4 CO NH MeCH(COOH)--                                                     2-49 4 CO NH HOOC--(CH.sub.2).sub.2 --                                        2-50 4 CO NH MeCH(COOMe)--                                                    2-51 4 CO NH 1-HOOC-iBu                                                       2-52 4 CO NH 1-MeOOC-iBu                                                      2-53 4 CO NH 1-HOOC-iPn                                                       2-54 4 CO NH 1-MeOOC-iPn                                                      2-55 4 CO NH 1-HOOC-2-Me-Bu                                                   2-56 4 CO NH 1-MeOOC-2-Me-Bu                                                  2-57 4 CO NH CH.sub.2 CH.sub.2 SO.sub.3 H                                     2-58 4 CO NH OH                                                               2-59 4 CO NH MeO                                                              2-60 4 CO NH EtO                                                              2-61 4 CO NH Pro                                                              2-62 4 CO NH iPrO                                                             2-63 4 CO NH BuO                                                              2-64 4 CO NH iBuO                                                             2-65 4 CO NH sBuO                                                             2-66 4 CO NH tBuO                                                             2-67 4 CO NH HxO                                                              2-68 4 CO NH PhO                                                              2-69 4 CO NH BnO                                                              2-70 4 CO NH Z-1                                                              2-71 4 CO NH Z-2                                                              2-72 4 CO NH Z-3                                                              2-73 4 CO NH Z-4                                                              2-74 4 CO NH Z-5                                                              2-75 4 CO NH Z-6                                                              2-76 4 CO NH Z-7                                                              2-77 4 CO NH Z-8                                                              2-78 4 CO NH Z-9                                                              2-79 4 CO NH Z-10                                                             2-80 4 CO NH Z-11                                                             2-81 4 CO NH Z-12                                                             2-82 4 CO NH 3-Py                                                             2-83 4 CO NH 4-Py                                                             2-84 4 CO N(Ac) H                                                             2-85 4 CO N(Ac) Ph                                                            2-86 4 CO N(Ac) 2-Me-Ph                                                       2-87 4 CO N(Ac) 4-Me-Ph                                                       2-88 4 CO N(Ac) 2,4-diMe-Ph                                                   2-89 4 CO N(Ac) 3,4-diMe-Ph                                                   2-90 4 CO N(Ac) 2-(CF.sub.3)Ph                                                2-91 4 CO N(Ac) 4-(CF.sub.3)Ph                                                2-92 4 CO N(Ac) 2-MeOPh                                                       2-93 4 CO N(Ac) 4-MeOPh                                                       2-94 4 CO N(Ac) 2-EtOPh                                                       2-95 4 CO N(Ac) 4-EtOPh                                                       2-96 4 CO N(Ac) 2-HOPh                                                        2-97 4 CO N(Ac) 4-HOPh                                                        2-98 4 CO N(Ac) 2-(HOOC)Ph                                                    2-99 4 CO N(Ac) 4-(HOOC)Ph                                                    2-100 4 CO N(Ac) 2-(MeOOC)Ph                                                  2-101 4 CO N(Ac) 4-(MeOOC)Ph                                                  2-102 4 CO N(Ac) 2-(EtOOC)Ph                                                  2-103 4 CO N(Ac) 4-(EtOOC)Ph                                                  2-104 4 CO N(Ac) 2-(tBuOOC)Ph                                                 2-105 4 CO N(Ac) 4-(tBuOOC)Ph                                                 2-106 4 CO N(Ac) 2-Cl-Ph                                                      2-107 4 CO N(Ac) 4-Cl-Ph                                                      2-108 4 CO N(Ac) 2-Br-Ph                                                      2-109 4 CO N(Ac) 4-Br-Ph                                                      2-110 4 CO N(Ac) 2-I-Ph                                                       2-111 4 CO N(Ac) 4-I-Ph                                                       2-112 4 CO N(Ac) 2-NO.sub.2 -Ph                                               2-113 4 CO N(Ac) 4-NO.sub.2 -Ph                                               2-114 4 CO N(Ac) 2-NH.sub.2 -Ph                                               2-115 4 CO N(Ac) 4-NH.sub.2 -Ph                                               2-116 4 CO N(Ac) 2-(HO.sub.3 S)Ph                                             2-117 4 CO N(Ac) 4-(HO.sub.3 S)Ph                                             2-118 4 CO N(Ac) 2-(NH.sub.2 O.sub.2 S)Ph                                     2-119 4 CO N(Ac) 4-(NH.sub.2 O.sub.2 S)Ph                                     2-120 4 CO N(Ac) 2-CN-Ph                                                      2-121 4 CO N(Ac) 4-CN-Ph                                                      2-122 4 CO N(Ac) 2-(HOCH.sub.2)Ph                                             2-123 4 CO N(Ac) 4-(HOCH.sub.2)Ph                                             2-124 4 CO N(Ac) Me                                                           2-125 4 CO N(Ac) Et                                                           2-126 4 CO N(Ac) Pr                                                           2-127 4 CO N(Ac) iPr                                                          2-128 4 CO N(Ac) Bu                                                           2-129 4 CO N(Ac) HOOCCH.sub.2 --                                              2-130 4 CO N(Ac) MeOOCCH.sub.2 --                                             2-131 4 CO N(Ac) MeCH(COOH)                                                   2-132 4 CO N(Ac) HOOC--(CH.sub.2).sub.2 --                                    2-133 4 CO N(Ac) MeCH(COOMe)                                                  2-134 4 CO N(Ac) 1-HOOC-iBu                                                   2-135 4 CO N(Ac) 1-MeOOC-iBu                                                  2-136 4 CO N(Ac) 1-HOOC-iPn                                                   2-137 4 CO N(Ac) 1-MeOOC-iPn                                                  2-138 4 CO N(Ac) 1-HOOC-2-Me-Bu                                               2-139 4 CO N(Ac) 1-MeOOC-2-Me-Bu                                              2-140 4 CO N(Ac) CH.sub.2 CH.sub.2 SO.sub.3 H                                 2-141 4 CO N(Ac) OH                                                           2-142 4 CO N(Ac) MeO                                                          2-143                                                                        4 CO N(Ac) EtO                                                                 2-144 4 CO N(Ac) PrO                                                          2-145 4 CO N(Ac) iPrO                                                         2-146 4 CO N(Ac) BuO                                                          2-147 4 CO N(Ac) iBuO                                                         2-148 4 CO N(Ac) sBuO                                                         2-149 4 CO N(Ac) tBuO                                                         2-150 4 CO N(Ac) HxO                                                          2-151 4 CO N(Ac) PhO                                                          2-152 4 CO N(Ac) BnO                                                          2-153 4 CO N(Ac) Z-1                                                          2-154 4 CO N(Ac) Z-2                                                          2-155 4 CO N(Ac) Z-3                                                          2-156 4 CO N(Ac) Z-4                                                          2-157 4 CO N(Ac) Z-5                                                          2-158 4 CO N(Ac) Z-6                                                          2-159 4 CO N(Ac) Z-7                                                          2-160 4 CO N(Ac) Z-8                                                          2-161 4 CO N(Ac) Z-9                                                          2-162 4 CO N(Ac) Z-10                                                         2-163 4 CO N(Ac) Z-11                                                         2-164 4 CO N(Ac) Z-12                                                         2-165 4 CO N(Ac) 3-Py                                                         2-166 4 CO N(Ac) 4-Py                                                         2-167 4 COO -- H                                                              2-168 4 COO -- Ph                                                             2-169 4 COO -- 2-Me-Ph                                                        2-170 4 COO -- 4-Me-Ph                                                        2-171 4 COO -- 2,4-diMe-Ph                                                    2-172 4 COO -- 3,4-diMe-Ph                                                    2-173 4 COO -- 2-(CF.sub.3)Ph                                                 2-174 4 COO -- 4-(CF.sub.3)Ph                                                 2-175 4 COO -- 2-MeOPh                                                        2-176 4 COO -- 4-MeOPh                                                        2-177 4 COO -- 2-EtOPh                                                        2-178 4 COO -- 4-EtOPh                                                        2-179 4 COO -- 2-HOPh                                                         2-180 4 COO -- 4-HOPh                                                         2-181 4 COO -- 2-(HOOC)Ph                                                     2-182 4 COO -- 4-(HOOC)Ph                                                     2-183 4 COO -- 2-(MeOOC)Ph                                                    2-184 4 COO -- 4-(MeOOC)Ph                                                    2-185 4 COO -- 2-(EtOOC)Ph                                                    2-186 4 COO -- 4-(EtOOC)Ph                                                    2-187 4 COO -- 2-(tBuOOC)Ph                                                   2-188 4 COO -- 4-(tBuOOC)Ph                                                   2-189 4 COO -- 2-Cl-Ph                                                        2-190 4 COO -- 4-Cl-Ph                                                        2-191 4 COO -- 2-Br-Ph                                                        2-192 4 COO -- 4-Br-Ph                                                        2-193 4 COO -- 2-I-Ph                                                         2-194 4 COO -- 4-I-Ph                                                         2-195 4 COO -- 2-NO.sub.2 -Ph                                                 2-196 4 COO -- 4-NO.sub.2 -Ph                                                 2-197 4 COO -- 2-NH.sub.2 -Ph                                                 2-198 4 COO -- 4-NH.sub.2 -Ph                                                 2-199 4 COO -- 2-(HO.sub.3 S)Ph                                               2-200 4 COO -- 4-(HO.sub.3 S)Ph                                               2-201 4 COO -- 2-(NH.sub.2 O.sub.2 S)Ph                                       2-202 4 COO -- 4-(NH.sub.2 O.sub.2 S)Ph                                       2-203 4 COO -- 2-CN-Ph                                                        2-204 4 COO -- 4-CN-Ph                                                        2-205 4 COO -- 2-(HOCH.sub.2)Ph                                               2-206 4 COO -- 4-(HOCH.sub.2)Ph                                               2-207 4 COO -- Me                                                             2-208 4 COO -- Et                                                             2-209 4 COO -- Pr                                                             2-210 4 COO -- iPr                                                            2-211 4 COO -- Bu                                                             2-212 4 COO -- HOOCCH.sub.2 --                                                2-213 4 COO -- HOOC--(CH.sub.2).sub.2 --                                      2-214 4 COO -- MeCH(COOMe)                                                    2-215 4 COO -- 1-HOOC-iBu                                                     2-216 4 COO -- 1-HOOC-iPn                                                     2-217 4 COO -- Z-1                                                            2-218 4 COO -- Z-2                                                            2-219 4 COO -- Z-3                                                            2-220 4 COO -- Z-4                                                            2-221 4 COO -- Z-5                                                            2-222 4 COO -- Z-6                                                            2-223 4 COO -- Z-7                                                            2-224 4 COO -- Z-8                                                            2-225 4 COO -- Z-9                                                            2-226 4 COO -- Z-10                                                           2-227 4 COO -- Z-11                                                           2-228 4 COO -- Z-12                                                           2-229 4 COO -- 3-Py                                                           2-230 4 COO -- 4-Py                                                           2-231 4 CONHCO -- H                                                           2-232 4 CONHCO -- Ph                                                          2-233 4 CONHCO -- 2-Me-Ph                                                     2-234 4 CONHCO -- 4-Me-Ph                                                     2-235 4 CONHCO -- 2,4-diMe-Ph                                                 2-236 4 CONHCO -- 3,4-diMe-Ph                                                 2-237 4 CONHCO -- 2-(CF.sub.3)Ph                                              2-238 4 CONHCO -- 4-(CF.sub.3)Ph                                              2-239 4 CONHCO -- 2-MeOPh                                                     2-240 4 CONHCO -- 4-MeOPh                                                     2-241 4 CONHCO -- 2-EtOPh                                                     2-242 4 CONHCO -- 4-EtOPh                                                     2-243 4 CONHCO -- 2-HOPh                                                      2-244 4 CONHCO -- 4-HOPh                                                      2-245 4 CONHCO -- 2-(HOOC)Ph                                                  2-246 4 CONHCO -- 4-(HOOC)Ph                                                  2-247 4 CONHCO -- 2-(MeOOC)Ph                                                 2-248 4 CONHCO -- 4-(MeOOC)Ph                                                 2-249 4 CONHCO -- 2-(EtOOC)Ph                                                 2-250 4 CONHCO -- 4-(EtOOC)Ph                                                 2-251 4 CONHCO -- 2-(tBuOOC)Ph                                                2-252 4 CONHCO -- 4-(tBuOOC)Ph                                                2-253 4 CONHCO -- 2-Cl-Ph                                                     2-254 4 CONHCO -- 4-Cl-Ph                                                     2-255 4 CONHCO -- 2-Br-Ph                                                     2-256 4 CONHCO -- 4-Br-Ph                                                     2-257 4 CONHCO -- 2-I-Ph                                                      2-258 4 CONHCO -- 4-I-Ph                                                      2-259 4 CONHCO -- 2-NO.sub.2 -Ph                                              2-260 4 CONHCO -- 4-NO.sub.2 -Ph                                              2-261 4 CONHCO -- 2-NH.sub.2 -Ph                                              2-262 4 CONHCO -- 4-NH.sub.2 -Ph                                              2-263 4 CONHCO -- 2-(HO.sub.3 S)Ph                                            2-264 4 CONHCO -- 4-(HO.sub.3 S)Ph                                            2-265 4 CONHCO -- 2-(NH.sub.2 O.sub.2 S)Ph                                    2-266 4 CONHCO -- 4-(NH.sub.2 O.sub.2 S)Ph                                    2-267 4 CONHCO -- 2-CN-Ph                                                     2-268 4 CONHCO -- 4-CN-Ph                                                     2-269 4 CONHCO -- 2-(HOCH.sub.2)Ph                                            2-270 4 CONHCO -- 4-(HOCH.sub.2)Ph                                            2-271 4 CONHCO -- Me                                                          2-272 4 CONHCO -- Et                                                          2-273 4 CONHCO -- Pr                                                          2-274 4 CONHCO -- iPr                                                         2-275 4 CONHCO -- Bu                                                          2-276 4 CONHCO -- HOOCCH.sub.2 --                                             2-277 4 CONHCO -- MeOOCCH.sub.2 --                                            2-278 4 CONHCO -- MeCH(COOH)                                                  2-279 4 CONHCO -- HOOC--(CH.sub.2).sub.2 --                                   2-280 4 CONHCO -- MeCH(COOMe)                                                 2-281 4 CONHCO -- 1-HOOC-iBu                                                  2-282 4 CONHCO -- 1-MeOOC-iBu                                                 2-283 4 CONHCO -- 1-HOOC-iPn                                                  2-284 4 CONHCO -- 1-MeOOC-iPn                                                 2-285 4 CONHCO -- 1-HOOC-2-Me-Bu                                              2-286 4 CONHCO -- 1-MeOOC-2-Me-Bu                                             2-287 4 CONHCO -- CH.sub.2 CH.sub.2 SO.sub.3 H                                2-288 4 CONHCO -- Z-1                                                         2-289 4 CONHCO -- Z-2                                                         2-290 4 CONHCO -- Z-3                                                         2-291 4 CONHCO -- Z-4                                                         2-292 4 CONHCO -- Z-5                                                         2-293 4 CONHCO -- Z-6                                                         2-294 4 CONHCO -- Z-7                                                         2-295 4 CONHCO -- Z-8                                                         2-296 4 CONHCO -- Z-9                                                         2-297 4 CONHCO -- Z-10                                                        2-298 4 CONHCO -- Z-11                                                        2-299 4 CONHCO -- Z-12                                                        2-300 4 CONHCO -- 3-Py                                                        2-301 4 CONHCO -- 4-Py                                                        2-302 4 CON(Ac)CO -- H                                                        2-303 4 CON(Ac)CO -- Ph                                                       2-304 4 CON(Ac)CO -- 2-Me-Ph                                                  2-305 4 CON(Ac)CO -- 4-Me-Ph                                                  2-306 4 CON(Ac)CO -- 2,4-diMe-Ph                                              2-307 4 CON(Ac)CO -- 3,4-diMe-Ph                                              2-308 4 CON(Ac)CO -- 2-(CF.sub.3)Ph                                           2-309 4 CON(Ac)CO -- 4-(CF.sub.3)Ph                                           2-310 4 CON(Ac)CO -- 2-MeOPh                                                  2-311 4 CON(Ac)CO -- 4-MeOPh                                                  2-312 4 CON(Ac)CO -- 2-EtOPh                                                  2-313 4 CON(Ac)CO -- 4-EtOPh                                                  2-314 4 CON(Ac)CO -- 2-HOPh                                                   2-315 4 CON(Ac)CO -- 4-HOPh                                                   2-316 4 CON(Ac)CO -- 2-(HOOC)Ph                                               2-317 4 CON(Ac)CO -- 4-(HOOC)Ph                                               2-318 4 CON(Ac)CO -- 2-(MeOOC)Ph                                              2-319 4 CON(Ac)CO -- 4-(MeOOC)Ph                                              2-320 4 CON(Ac)CO -- 2-(EtOOC)Ph                                              2-321 4 CON(Ac)CO -- 4-(EtOOC)Ph                                              2-322 4 CON(Ac)CO -- 2-(tBuOOC)Ph                                             2-323 4 CON(Ac)CO -- 4-(tBuOOC)Ph                                             2-324 4 CON(Ac)CO -- 2-Cl-Ph                                                  2-325 4 CON(Ac)CO -- 4-Cl-Ph                                                  2-326 4 CON(Ac)CO -- 2-Br-Ph                                                  2-327 4 CON(Ac)CO -- 4-Br-Ph                                                  2-328 4 CON(Ac)CO -- 2-I-Ph                                                   2-329 4 CON(Ac)CO -- 4-I-Ph                                                   2-330 4 CON(Ac)CO -- 2-NO.sub.2 -Ph                                           2-331 4 CON(Ac)CO -- 4-NO.sub.2 -Ph                                           2-332 4 CON(Ac)CO -- 2-NH.sub.2 -Ph                                           2-333 4 CON(Ac)CO -- 4-NH.sub.2 -Ph                                           2-334 4 CON(Ac)CO -- 2-(HO.sub.3 S)Ph                                         2-335 4 CON(Ac)CO -- 4-(HO.sub.3 S)Ph                                         2-336 4 CON(Ac)CO -- 2-(NH.sub.2 O.sub.2 S)Ph                                 2-337 4 CON(Ac)CO -- 4-(NH.sub.2 O.sub.2 S)Ph                                 2-338 4 CON(Ac)CO -- 2-CN-Ph                                                  2-339 4 CON(Ac)CO -- 4-CN-Ph                                                  2-340 4 CON(Ac)CO -- 2-(HOCH.sub.2)Ph                                         2-341 4 CON(Ac)CO -- 4-(HOCH.sub.2)Ph                                         2-342 4 CON(Ac)CO -- Me                                                       2-343 4 CON(Ac)CO -- Et                                                       2-344 4 CON(Ac)CO -- Pr                                                       2-345 4 CON(Ac)CO -- iPr                                                      2-346 4 CON(Ac)CO -- Bu                                                       2-347 4 CON(Ac)CO -- HOOCCH.sub.2 --                                          2-348 4 CON(Ac)CO -- MeOOCCH.sub.2 --                                         2-349 4 CON(Ac)CO -- MeCH(COOH)                                               2-350 4 CON(Ac)CO -- HOOC--(CH.sub.2).sub.2 --                                2-351 4 CON(Ac)CO -- MeCH(COOMe)                                              2-352 4 CON(Ac)CO -- 1-HOOC-iBu                                               2-353 4 CON(Ac)CO -- 1-MeOOC-iBu                                              2-354 4 CON(Ac)CO -- 1-HOOC-iPn                                               2-355 4 CON(Ac)CO -- I-MeOOC-iPn                                              2-356 4 CON(Ac)CO -- 1-HOOC-2-Me-Bu                                           2-357 4 CON(Ac)CO -- 1-MeOOC-2-Me-Bu                                          2-358 4 CON(Ac)CO -- CH.sub.2 CH.sub.2 SO.sub.3 H                             2-359 4 CON(Ac)CO -- Z-1                                                      2-360 4 CON(Ac)CO -- Z-2                                                      2-361 4 CON(Ac)CO -- Z-3                                                      2-362 4 CON(Ac)CO -- Z-4                                                      2-363 4 CON(Ac)CO -- Z-5                                                      2-364 4 CON(Ac)CO -- Z-6                                                      2-365 4 CON(Ac)CO -- Z-7                                                      2-366 4 CON(Ac)CO -- Z-8                                                      2-367 4 CON(Ac)CO -- Z-9                                                      2-368 4 CON(Ac)CO -- Z-10                                                     2-369 4 CON(Ac)CO -- Z-11                                                     2-370 4 CON(Ac)CO -- Z-12                                                     2-371 4 CON(Ac)CO -- 3-Py                                                     2-372 4 CON(Ac)CO -- 4-Py                                                     2-373 4 CONHCO NH H                                                           2-374 4 CONHCO NH Ph                                                          2-375 4 CONHCO NH 2-Me-Ph                                                     2-376 4 CONHCO NH 4-Me-Ph                                                     2-377 4 CONHCO NH 2,4-diMe-Ph                                                 2-378 4 CONHCO NH 3,4-diMe-Ph                                                 2-379 4 CONHCO NH 2-(CF.sub.3)Ph                                              2-380 4 CONHCO NH 4-(CF.sub.3)Ph                                              2-381 4 CONHCO NH 2-MeOPh                                                     2-382 4 CONHCO NH 4-MeOPh                                                     2-383 4 CONHCO NH 2-EtOPh                                                     2-384 4 CONHCO NH 4-EtOPh                                                     2-385 4 CONHCO NH 2-HOPh                                                      2-386 4 CONHCO NH 4-HOPh                                                      2-387 4 CONHCO NH 2-(HOOC)Ph                                                  2-388 4 CONHCO NH 4-(HOOC)Ph                                                  2-389 4 CONHCO NH 2-(MeOOC)Ph                                                 2-390 4 CONHCO NH 4-(MeOOC)Ph                                                 2-391 4 CONHCO NH 2-(EtOOC)Ph                                                 2-392 4 CONHCO NH 4-(EtOOC)Ph                                                 2-393 4 CONHCO NH 2-(tBuOOC)Ph                                                2-394 4 CONHCO NH 4-(tBuOOC)Ph                                                2-395 4 CONHCO NH 2-Cl-Ph                                                     2-396 4 CONHCO NH 4-Cl-Ph                                                     2-397 4 CONHCO NH 2-Br-Ph                                                     2-398 4 CONHCO NH 4-Br-Ph                                                     2-399 4 CONHCO NH 2-I-Ph                                                      2-400 4 CONHCO NH 4-I-Ph                                                      2-401 4 CONHCO NH 2-NO.sub.2 -Ph                                              2-402 4 CONHCO NH 4-NO.sub.2 -Ph                                              2-403 4 CONHCO NH 2-NH.sub.2 -Ph                                              2-404 4 CONHCO NH 4-NH.sub.2 -Ph                                              2-405 4 CONHCO NH 2-(HO.sub.3 S)Ph                                            2-406 4 CONHCO NH 4-(HO.sub.3 S)Ph                                            2-407 4 CONHCO NH 2-(NH.sub.2 O.sub.2 S)Ph                                    2-408 4 CONHCO NH 4-(NH.sub.2 O.sub.2 S)Ph                                    2-409 4 CONHCO NH 2-CN-Ph                                                     2-410 4 CONHCO NH 4-CN-Ph                                                     2-411 4 CONHCO NH 2-(HOCH.sub.2)Ph                                            2-412 4 CONHCO NH 4-(HOCH.sub.2)Ph                                            2-413 4 CONHCO NH Me                                                          2-414 4 CONHCO NH Et                                                          2-415 4 CONHCO NH Pr                                                          2-416 4 CONHCO NH iPr                                                         2-417 4 CONHCO NH Bu                                                          2-418 4 CONHCO NH HOOCCH.sub.2 --                                             2-419 4 CONHCO NH MeOOCCH.sub.2 --                                            2-420 4 CONHCO NH MeCH(COOH)                                                  2-421 4 CONHCO NH HOOC--(CH.sub.2).sub.2 --                                   2-422 4 CONHCO NH MeCH(COOMe)                                                 2-423 4 CONHCO NH 1-HOOC-iBu                                                  2-424 4 CONHCO NH 1-MeOOC-iBu                                                 2-425 4 CONHCO NH 1-HOOC-iPn                                                  2-426 4 CONHCO NH 1-MeOOC-iPn                                                 2-427 4 CONHCO NH 1-HOOC-2-Me-Bu                                              2-428 4 CONHCO NH 1-MeOOC-2-Me-Bu                                             2-429 4 CONHCO NH CH.sub.2 CH.sub.2 SO.sub.3 H                                2-430 4 CONHCO NH HO                                                          2-431 4 CONHCO NH MeO                                                         2-432 4 CONHCO NH EtO                                                         2-433 4 CONHCO NH PrO                                                         2-434 4 CONHCO NH iPrO                                                        2-435 4 CONHCO NH BuO                                                         2-436 4 CONHCO NH iBuO                                                        2-437 4 CONHCO NH sBuO                                                        2-438 4 CONHCO NH tBuO                                                        2-439 4 CONHCO NH HxO                                                         2-440 7 CONHCO NH PhO                                                         2-441 4 CONHCO NH BnO                                                         2-442 4 CONHCO NH Z-1                                                         2-443 4 CONHCO NH Z-2                                                         2-444 4 CONHCO NH Z-3                                                         2-445 4 CONHCO NH Z-4                                                         2-446 4 CONHCO NH Z-5                                                         2-447 4 CONHCO NH Z-6                                                         2-448 4 CONHCO NH Z-7                                                         2-449 4 CONHCO NH Z-8                                                         2-450 4 CONHCO NH Z-9                                                         2-451 4 CONHCO NH Z-10                                                        2-452 4 CONHCO NH Z-11                                                        2-453 4 CONHCO NH Z-12                                                        2-454 4 CONHCO NH 3-Py                                                        2-455 4 CONHCO NH 4-Py                                                        2-456 4 CONHSO.sub.2 -- H                                                     2-457 4 CONHSO.sub.2 -- Ph                                                    2-458 4 CONHSO.sub.2 -- 2-Me-Ph                                               2-459 4 CONHSO.sub.2 -- 4-Me-Ph                                               2-460 4 CONHSO.sub.2 -- 2,4-diMe-Ph                                           2-461 4 CONHSO.sub.2 -- 3,4-diMe-Ph                                           2-462 4 CONHSO.sub.2 -- 2-(CF.sub.3)Ph                                        2-463 4 CONHSO.sub.2 -- 4-(CF.sub.3)Ph                                        2-464 4 CONHSO.sub.2 -- 2-MeOPh                                               2-465 4 CONHSO.sub.2 -- 4-MeOPh                                               2-466 4 CONHSO.sub.2 -- 2-EtOPh                                               2-467 4 CONHSO.sub.2 -- 4-EtOPh                                               2-468 4 CONHSO.sub.2 -- 2-HOPh                                                2-469 4 CONHSO.sub.2 -- 4-HOPh                                                2-470 4 CONHSO.sub.2 -- 2-(HOOC)Ph                                            2-471 4 CONHSO.sub.2 -- 4-(HOOC)Ph                                            2-472 4 CONHSO.sub.2 -- 2-(MeOOC)Ph                                           2-473 4 CONHSO.sub.2 -- 4-(MeOOC)Ph                                           2-474 4 CONHSO.sub.2 -- 2-(EtOOC)Ph                                           2-475 4 CONHSO.sub.2 -- 4-(EtOOC)Ph                                           2-476 4 CONHSO.sub.2 -- 2-(tBuOOC)Ph                                          2-477 4 CONHSO.sub.2 -- 4-(tBuOOC)Ph                                          2-478 4 CONHSO.sub.2 -- 2-Cl-Ph                                               2-479 4 CONHSO.sub.2 -- 4-Cl-Ph                                               2-480 4 CONHSO.sub.2 -- 2-Br-Ph                                               2-481 4 CONHSO.sub.2 -- 4-Br-Ph                                               2-482 4 CONHSO.sub.2 -- 2-I-Ph                                                2-483 4 CONHSO.sub.2 -- 4-I-Ph                                                2-484 4 CONHSO.sub.2 -- 2-NO.sub.2 -Ph                                        2-485 4 CONHSO.sub.2 -- 4-NO.sub.2 -Ph                                        2-486 4 CONHSO.sub.2 -- 2-NH.sub.2 -Ph                                        2-487 4 CONHSO.sub.2 -- 4-NH.sub.2 -Ph                                        2-488 4 CONHSO.sub.2 -- 2-(HO.sub.3 S)Ph                                      2-489 4 CONHSO.sub.2 -- 4-(HO.sub.3 S)Ph                                      2-490 4 CONHSO.sub.2 -- 2-(NH.sub.2 O.sub.2 S)Ph                              2-491 4 CONHSO.sub.2 -- 4-(NH.sub.2 O.sub.2 S)Ph                              2-492 4 CONHSO.sub.2 -- 2-CN-Ph                                               2-493 4 CONHSO.sub.2 -- 4-CN-Ph                                               2-494 4 CONHSO.sub.2 -- 2-(HOCH.sub.2)Ph                                      2-495 4 CONHSO.sub.2 -- 4-(HOCH.sub.2)Ph                                      2-496 4 CONHSO.sub.2 -- Me                                                    2-497 4 CONHSO.sub.2 -- Et                                                    2-498 4 CONHSO.sub.2 -- Pr                                                    2-499 4 CONHSO.sub.2 -- iPr                                                   2-500 4 CONHSO.sub.2 -- Bu                                                    2-501 4 CONHSO.sub.2 -- HOOCCH.sub.2 --                                       2-502 4 CONHSO.sub.2 -- MeOOCCH.sub.2 --                                      2-503 4 CONHSO.sub.2 -- MeCH(COOH)                                            2-504 4 CONHSO.sub.2 -- HOOC--(CH.sub.2).sub.2 --                             2-505 4 CONHSO.sub.2 -- MeCH(COOMe)                                           2-506 4 CONHSO.sub.2 -- 1-HOOC-iBu                                            2-507 4 CONHSO.sub.2 -- 1-MeOOC-iBu                                           2-508 4 CONHSO.sub.2 -- 1-HOOC-iPn                                            2-509 4 CONHSO.sub.2 -- 1-MeOOC-iPn                                           2-510 4 CONHSO.sub.2 -- 1-HOOC-2-Me-Bu                                        2-511 4 CONHSO.sub.2 -- 1-MeOOC-2-Me-Bu                                       2-512 4 CONHSO.sub.2 -- CH.sub.2 CH.sub.2 SO.sub.3 H                          2-513 4 CONHSO.sub.2 -- OH                                                    2-514 4 CONHSO.sub.2 -- MeO                                                   2-515 4 CONHSO.sub.2 -- EtO                                                   2-516 4 CONHSO.sub.2 -- PrO                                                   2-517 4 CONHSO.sub.2 -- iPrO                                                  2-518 4 CONHSO.sub.2 -- BuO                                                   2-519 4 CONHSO.sub.2 -- iBuO                                                  2-520 4 CONHSO.sub.2 -- sBuO                                                  2-521 4 CONHSO.sub.2 -- tBuO                                                  2-522 4 CONHSO.sub.2 -- HxO                                                   2-523 4 CONHSO.sub.2 -- PhO                                                   2-524 4 CONHSO.sub.2 -- BnO                                                   2-525 4 CONHSO.sub.2 -- Z-1                                                   2-526 4 CONHSO.sub.2 -- Z-2                                                   2-527 4 CONHSO.sub.2 -- Z-3                                                   2-528 4 CONHSO.sub.2 -- Z-4                                                   2-529 4 CONHSO.sub.2 -- Z-5                                                   2-530 4 CONHSO.sub.2 -- Z-6                                                   2-531 4 CONHSO.sub.2 -- Z-7                                                   2-532 4 CONHSO.sub.2 -- Z-8                                                   2-533 4 CONHSO.sub.2 -- Z-9                                                   2-534 4 CONHSO.sub.2 -- Z-10                                                  2-535 4 CONHSO.sub.2 -- Z-11                                                  2-536 4 CONHSO.sub.2 -- Z-12                                                  2-537 4 CONHSO.sub.2 -- 3-Py                                                  2-538 4 CONHSO.sub.2 -- 4-Py                                                  2-539 4 CONHSO.sub.2 NH H                                                     2-540 4 CONHSO.sub.2 NH Ph                                                    2-541 4 CONHSO.sub.2 NH 2-Me-Ph                                               2-542 4 CONHSO.sub.2 NH 4-Me-Ph                                               2-543 4 CONHSO.sub.2 NH 2,4-diMe-Ph                                           2-544 4 CONHSO.sub.2 NH 3,4-diMe-Ph                                           2-545 4 CONHSO.sub.2 NH 2-(CF.sub.3)Ph                                        2-546 4 CONHSO.sub.2 NH 4-(CF.sub.3)Ph                                        2-547 4 CONHSO.sub.2 NH 2-MeOPh                                               2-548 4 CONHSO.sub.2 NH 4-MeOPh                                               2-549 4 CONHSO.sub.2 NH 2-EtOPh                                               2-550 4 CONHSO.sub.2 NH 4-EtOPh                                               2-551 4 CONHSO.sub.2 NH 2-HOPh                                                2-552 4 CONHSO.sub.2 NH 4-HOPh                                                2-553 4 CONHSO.sub.2 NH 2-(HOOC)Ph                                            2-554 4 CONHSO.sub.2 NH 4-(HOOC)Ph                                            2-555 4 CONHSO.sub.2 NH 2-(MeOOC)Ph                                           2-556 4 CONHSO.sub.2 NH 4-(MeOOC)Ph                                           2-557 4 CONHSO.sub.2 NH 2-(EtOOC)Ph                                           2-558 4 CONHSO.sub.2 NH 4-(EtOOC)Ph                                           2-559 4 CONHSO.sub.2 NH 2-(tBuOOC)Ph                                          2-560 4 CONHSO.sub.2 NH 4-(tBuOOC)Ph                                          2-561 4 CONHSO.sub.2 NH 2-Cl-Ph                                               2-562 4 CONHSO.sub.2 NH 4-Cl-Ph                                               2-563 4 CONHSO.sub.2 NH 2-Br-Ph                                               2-564 4 CONHSO.sub.2 NH 4-Br-Ph                                               2-565 4 CONHSO.sub.2 NH 2-I-Ph                                                2-566 4 CONHSO.sub.2 NH 4-I-Ph                                                2-567 4 CONHSO.sub.2 NH 2-NO.sub.2 -Ph                                        2-568 4 CONHSO.sub.2 NH 4-NO.sub.2 -Ph                                        2-569 4 CONHSO.sub.2 NH 2-NH.sub.2 -Ph                                        2-570 4 CONHSO.sub.2 NH 4-NH.sub.2 -Ph                                        2-571 4 CONHSO.sub.2 NH 2-(HO.sub.3 S)Ph                                      2-572 4 CONHSO.sub.2 NH 4-(HO.sub.3 S)Ph                                      2-573 4 CONHSO.sub.2 NH 2-(NH.sub.2 O.sub.2 S)Ph                              2-574 4 CONHSO.sub.2 NH 4-(NH.sub.2 O.sub.2 S)Ph                              2-575 4 CONHSO.sub.2 NH 2-CN-Ph                                               2-576 4 CONHSO.sub.2 NH 4-CN-Ph                                               2-577 4 CONHSO.sub.2 NH 2-(HOCH.sub.2)Ph                                      2-578 4 CONHSO.sub.2 NH 4-(HOCH.sub.2)Ph                                      2-579 4 CONHSO.sub.2 NH Me                                                    2-580 4 CONHSO.sub.2 NH Et                                                    2-581 4 CONHSO.sub.2 NH Pr                                                    2-582 4 CONHSO.sub.2 NH iPr                                                   2-583 4 CONHSO.sub.2 NH Bu                                                    2-584 4 CONHSO.sub.2 NH HOOCCH.sub.2 --                                       2-585 4 CONHSO.sub.2 NH MeOOCCH.sub.2 --                                      2-586 4 CONHSO.sub.2 NH MeCH(COOH)                                            2-587 4 CONHSO.sub.2 NH HOOC--(CH.sub.2).sub.2 --                             2-588 4 CONHSO.sub.2 NH MeCH(COOMe)                                           2-589 4 CONHSO.sub.2 NH 1-HOOC-iBu                                            2-590 4 CONHSO.sub.2 NH 1-MeOOC-iBu                                           2-591 4 CONHSO.sub.2 NH 1-HOOC-iPn                                            2-592 4 CONHSO.sub.2 NH 1-MeOOC-iPn                                           2-593 4 CONHSO.sub.2 NH 1-HOOC-2-Me-Bu                                        2-594 4 CONHSO.sub.2 NH 1-MeOOC-2-Me-Bu                                       2-595 4 CONHSO.sub.2 NH CH.sub.2 CH.sub.2 SO.sub.3 H                          2-596 4 CONHSO.sub.2 NH OH                                                    2-597 4 CONHSO.sub.2 NH MeO                                                   2-598 4 CONHSO.sub.2 NH EtO                                                   2-599 4 CONHSO.sub.2 NH PrO                                                   2-600 4 CONHSO.sub.2 NH iPrO                                                  2-601 4 CONHSO.sub.2 NH BuO                                                   2-602 4 CONHSO.sub.2 NH iBuO                                                  2-603 4 CONHSO.sub.2 NH sBuO                                                  2-604 4 CONHSO.sub.2 NH tBuO                                                  2-605 4 CONHSO.sub.2 NH HxO                                                   2-606 4 CONHSO.sub.2 NH PhO                                                   2-607 4 CONHSO.sub.2 NH BnO                                                   2-608 4 CONHSO.sub.2 NH Z-1                                                   2-609 4 CONHSO.sub.2 NH Z-2                                                   2-610 4 CONHSO.sub.2 NH Z-3                                                   2-611 4 CONHSO.sub.2 NH Z-4                                                   2-612 4 CONHSO.sub.2 NH Z-5                                                   2-613 4 CONHSO.sub.2 NH Z-6                                                   2-614 4 CONHSO.sub.2 NH Z-7                                                   2-615 4 CONHSO.sub.2 NH Z-8                                                   2-616 4 CONHSO.sub.2 NH Z-9                                                   2-617 4 CONHSO.sub.2 NH Z-10                                                  2-618 4 CONHSO.sub.2 NH Z-11                                                  2-619 4 CONHSO.sub.2 NH Z-12                                                  2-620 4 CONHSO.sub.2 NH 3-Py                                                  2-621 4 CONHSO.sub.2 NH 4-Py                                                  2-622 4 NHCO -- H                                                             2-623 4 NHCO -- Ph                                                            2-624 4 NHCO -- 2-Me-Ph                                                       2-625 4 NHCO -- 4-Me-Ph                                                       2-626 4 NHCO -- 2,4-diMe-Ph                                                   2-627 4 NHCO -- 3,4-diMe-Ph                                                   2-628 4 NHCO -- 2-(CF.sub.3)Ph                                                2-629 4 NHCO -- 4-(CF.sub.3)Ph                                                2-630 4 NHCO -- 2-MeOPh                                                       2-631 4 NHCO -- 4-MeOPh                                                       2-632 4 NHCO -- 2-EtOPh                                                       2-633 4 NHCO -- 4-EtOPh                                                       2-634 4 NHCO -- 2-HOPh                                                        2-635 4 NHCO -- 4-HOPh                                                        2-636 4 NHCO -- 2-(HOOC)Ph                                                    2-637 4 NHCO -- 4-(HOOC)Ph                                                    2-638 4 NHCO -- 2-(MeOOC)Ph                                                   2-639 4 NHCO -- 4-(MeOOC)Ph                                                   2-640 4 NHCO -- 2-(EtOOC)Ph                                                   2-641 4 NHCO -- 4-(EtOOC)Ph                                                   2-642 4 NHCO -- 2-(tBuOOC)Ph                                                  2-643 4 NHCO -- 4-(tBuOOC)Ph                                                  2-644 4 NHCO -- 2-Cl-Ph                                                       2-645 4 NHCO -- 4-Cl-Ph                                                       2-646 4 NHCO -- 2-Br-Ph                                                       2-647 4 NHCO -- 4-Br-Ph                                                       2-648 4 NHCO -- 2-I-Ph                                                        2-649 4 NHCO -- 4-I-Ph                                                        2-650 4 NHCO -- 2-NO.sub.2 -Ph                                                2-651 4 NHCO -- 4-NO.sub.2 -Ph                                                2-652 4 NHCO -- 2-NH.sub.2 -Ph                                                2-653 4 NHCO -- 4-NH.sub.2 -Ph                                                2-654 4 NHCO -- 2-(HO.sub.3 S)Ph                                              2-655 4 NHCO -- 4-(HO.sub.3 S)Ph                                              2-656 4 NHCO -- 2-(NH.sub.2 O.sub.2 S)Ph                                      2-657 4 NHCO -- 4-(NH.sub.2 O.sub.2 S)Ph                                      2-658 4 NHCO -- 2-CN-Ph                                                       2-659 4 NHCO -- 4-CN-Ph                                                       2-660 4 NHCO -- 2-(HOCH.sub.2)Ph                                              2-661 4 NHCO -- 4-(HOCH.sub.2)Ph                                              2-662 4 NHCO -- Me                                                            2-663 4 NHCO -- Et                                                            2-664 4 NHCO -- Pr                                                            2-665 4 NHCO -- iPr                                                           2-666 4 NHCO -- Bu                                                            2-667 4 NHCO -- HOOCCH.sub.2 --                                               2-668 4 NHCO -- MeOOCCH.sub.2 --                                              2-669 4 NHCO -- MeCH(COOH)                                                    2-670 4 NHCO -- HOOC--(CH.sub.2).sub.2 --                                     2-671 4 NHCO -- MeCH(COOMe)                                                   2-672 4 NHCO -- 1-HOOC-iBu                                                    2-673 4 NHCO -- 1-HOOC-iPn                                                    2-674 4 NHCO -- 1-HOOC-2-Me-Bu                                                2-675 4 NHCO -- CH.sub.2 CH.sub.2 SO.sub.3 H                                  2-676 4 NHCO -- MeO                                                           2-677 4 NHCO -- EtO                                                           2-678 4 NHCO -- PrO                                                           2-679 4 NHCO -- Z-1                                                           2-680 4 NHCO -- Z-2                                                           2-681 4 NHCO -- Z-3                                                           2-682 4 NHCO -- Z-4                                                           2-683 4 NHCO -- Z-5                                                           2-684 4 NHCO -- Z-6                                                           2-685 4 NHCO -- Z-7                                                           2-686 4 NHCO -- Z-8                                                           2-687 4 NHCO -- Z-9                                                           2-688 4 NHCO -- Z-10                                                          2-689 4 NHCO -- Z-11                                                          2-690 4 NHCO -- Z-12                                                          2-691 4 NHCO -- 3-Py                                                          2-692 4 NHCO -- 4-Py                                                          2-693 4 NHCO NH H                                                             2-694 4 NHCO NH Ph                                                            2-695 4 NHCO NH 2-Me-Ph                                                       2-696 4 NHCO NH 4-Me-Ph                                                       2-697 4 NHCO NH 2,4-diMe-Ph                                                   2-698 4 NHCO NH 3,4-diMe-Ph                                                   2-699 4 NHCO NH 2-(CF.sub.3)Ph                                                2-700 4 NHCO NH 4-(CF.sub.3)Ph                                                2-701 4 NHCO NH 2-MeOPh                                                       2-702 4 NHCO NH 4-MeOPh                                                       2-703 4 NHCO NH 2-EtOPh                                                       2-704 4 NHCO NH 4-EtOPh                                                       2-705 4 NHCO NH 2-HOPh                                                        2-706 4 NHCO NH 4-HOPh                                                        2-707 4 NHCO NH 2-(HOOC)Ph                                                    2-708 4 NHCO NH 4-(HOOC)Ph                                                    2-709 4 NHCO NH 2-(MeOOC)Ph                                                   2-710 4 NHCO NH 4-(MeOOC)Ph                                                   2-711 4 NHCO NH 2-(EtOOC)Ph                                                   2-712 4 NHCO NH 4-(EtOOC)Ph                                                   2-713 4 NHCO NH 2-(tBuOOC)Ph                                                  2-714 4 NHCO NH 4-(tBuOOC)Ph                                                  2-715 4 NHCO NH 2-Cl-Ph                                                       2-716 4 NHCO NH 4-Cl-Ph                                                       2-717 4 NHCO NH 2-Br-Ph                                                       2-718 4 NHCO NH 4-Br-Ph                                                       2-719 4 NHCO NH 2-I-Ph                                                        2-720 4 NHCO NH 4-I-Ph                                                        2-721 4 NHCO NH 2-NO.sub.2 -Ph                                                2-722 4 NHCO NH 4-NO.sub.2 -Ph                                                2-723 4 NHCO NH 2-NH.sub.2 -Ph                                                2-724 4 NHCO NH 4-NH.sub.2 -Ph                                                2-725 4 NHCO NH 2-(HO.sub.3 S)Ph                                              2-726 4 NHCO NH 4-(HO.sub.3 S)Ph                                              2-727 4 NHCO NH 2-(NH.sub.2 O.sub.2 S)Ph                                      2-728 4 NHCO NH 4-(NH.sub.2 O.sub.2 S)Ph                                      2-729 4 NHCO NH 2-CN-Ph                                                       2-730 4 NHCO NH 4-CN-Ph                                                       2-731 4 NHCO NH 2-(HOCH.sub.2)Ph                                              2-732 4 NHCO NH 4-(HOCH.sub.2)Ph                                              2-733 4 NHCO NH Me                                                            2-734 4 NHCO NH Et                                                            2-735 4 NHCO NH Pr                                                            2-736 4 NHCO NH iPr                                                           2-737 4 NHCO NH Bu                                                            2-738 4 NHCO NH HOOCCH.sub.2 --                                               2-739 4 NHCO NH MeOOCCH.sub.2 --                                              2-740 4 NHCO NH MeCH(COOH)                                                    2-741 4 NHCO NH HOOC--(CH.sub.2).sub.2 --                                     2-742 4 NHCO NH MeCH(COOMe)                                                   2-743 4 NHCO NH 1-HOOC-iBu                                                    2-744 4 NHCO NH 1-MeOOC-iBu                                                   2-745 4 NHCO NH 1-HOOC-iPn                                                    2-746 4 NHCO NH 1-MeOOC-iPn                                                   2-747 4 NHCO NH 1-HOOC-2-Me-Bu                                                2-748 4 NHCO NH 1-MeOOC-2-Me-Bu                                               2-749 4 NHCO NH CH.sub.2 CH.sub.2 SO.sub.3 H                                  2-750 4 NHCO NH OH                                                            2-751 4 NHCO NH MeO                                                           2-752 4 NHCO NH EtO                                                           2-753 4 NHCO NH PrO                                                           2-754 4 NHCO NH iPrO                                                          2-755 4 NHCO NH BuO                                                           2-756 4 NHCO NH iBuO                                                          2-757 4 NHCO NH sBuO                                                          2-758 4 NHCO NH tBuO                                                          2-759 4 NHCO NH HxO                                                           2-760 4 NHCO NH PhO                                                           2-761 4 NHCO NH BnO                                                           2-762 4 NHCO NH Z-1                                                           2-763 4 NHCO NH Z-2                                                           2-764 4 NHCO NH Z-3                                                           2-765 4 NHCO NH Z-4                                                           2-766 4 NHCO NH Z-5                                                           2-767 4 NHCO NH Z-6                                                           2-768 4 NHCO NH Z-7                                                           2-769 4 NHCO NH Z-8                                                           2-770 4 NHCO NH Z-9                                                           2-771 4 NHCO NH Z-10                                                          2-772 4 NHCO NH Z-11                                                          2-773 4 NHCO NH Z-12                                                          2-774 4 NHCO NH 3-Py                                                          2-775 4 NHCO NH 4-Py                                                          2-776 4 NHCO NMe Ph                                                           2-777 4 NHCO NMe 2-Me-Ph                                                      2-778 4 NHCO NMe 4-Me-Ph                                                      2-779 4 NHCO NMe 2,4-diMe-Ph                                                  2-780 4 NHCO NMe 3,4-diMe-Ph                                                  2-781 4 NHCO NMe 2-(CF.sub.3)Ph                                               2-782 4 NHCO NMe 4-(CF.sub.3)Ph                                               2-783 4 NHCO NMe 2-MeOPh                                                      2-784 4 NHCO NMe 4-MeOPh                                                      2-785 4 NHCO NMe 2-EtOPh                                                      2-786 4 NHCO NMe 4-EtOPh                                                      2-787 4 NHCO NMe 2-HOPh                                                       2-788 4 NHCO NMe 4-HOPh                                                       2-789 4 NHCO NMe 2-(HOOC)Ph                                                   2-790 4 NHCO NMe 4-(HOOC)Ph                                                   2-791 4 NHCO NMe 2-(MeOOC)Ph                                                  2-792 4 NHCO NMe 4-(MeOOC)Ph                                                  2-793 4 NHCO NMe 2-(EtOOC)Ph                                                  2-794 4 NHCO NMe 4-(EtOOC)Ph                                                  2-795 4 NHCO NMe 2-(tBuOOC)Ph                                                 2-796 4 NHCO NMe 4-(tBuOOC)Ph                                                 2-797 4 NHCO NMe 2-Cl-Ph                                                      2-798 4 NHCO NMe 4-Cl-Ph                                                      2-799 4 NHCO NMe 2-Br-Ph                                                      2-800 4 NHCO NMe 4-Br-Ph                                                      2-801 4 NHCO NMe 2-I-Ph                                                       2-802 4 NHCO NMe 4-I-Ph                                                       2-803 4 NHCO NMe 2-NO.sub.2 -Ph                                               2-804 4 NHCO NMe 4-NO.sub.2 -Ph                                               2-805 4 NHCO NMe 2-NH.sub.2 -Ph                                               2-806 4 NHCO NMe 4-NH.sub.2 -Ph                                               2-807 4 NHCO NMe 2-(HO.sub.2 S)Ph                                             2-808 4 NHCO NMe 4-(HO.sub.3 S)Ph                                             2-809 4 NHCO NMe 2-(NH.sub.2 O.sub.2 S)Ph                                     2-810 4 NHCO NMe 4-(NH.sub.2 O.sub.2 S)Ph                                     2-811 4 NHCO NMe 2-CN-Ph                                                      2-812 4 NHCO NMe 4-CN-Ph                                                      2-813 4 NHCO NMe 2-(HOCH.sub.2)Ph                                             2-814 4 NHCO NMe 4-(HOCH.sub.2)Ph                                             2-815 4 NHCO NMe Me                                                           2-816 4 NHCO NMe Et                                                           2-817 4 NHCO NMe Pr                                                           2-818 4 NHCO NMe iPr                                                          2-819 4 NHCO NMe Bu                                                           2-820 4 NHCO NMe HOOCCH.sub.2 --                                              2-821 4 NHCO NMe MeOOCCH.sub.2 --                                             2-822 4 NHCO NMe MeCH(COOH)                                                   2-823 4 NHCO NMe HOOC--(CH.sub.2).sub.2 --                                    2-824 4 NHCO NMe MeCH(COOMe)                                                  2-825 4 NHCO NMe 1-HOOC-iBu                                                   2-826 4 NHCO NMe 1-MeOOC-iBu                                                  2-827 4 NHCO NMe 1-HOOC-iPn                                                   2-828 4 NHCO NMe 1-MeOOC-iPn                                                  2-829 4 NHCO NMe 1-HOOC-2-Me-Bu                                               2-830 4 NHCO NMe 1-MeOOC-2-Me-Bu                                              2-831 4 NHCO NMe CH.sub.2 CH.sub.2 SO.sub.3 H                                 2-832 4 NHCO NMe OH                                                           2-833 4 NHCO NMe MeO                                                          2-834 4 NHCO NMe EtO                                                          2-835 4 NHCO NMe PrO                                                          2-836 4 NHCO NMe iPrO                                                         2-837 4 NHCO NMe BuO                                                          2-838 4 NHCO NMe iBuO                                                         2-839 4 NHCO NMe sBuO                                                         2-840 4 NHCO NMe tBuO                                                         2-841 4 NHCO NMe HxO                                                          2-842 4 NHCO NMe PhO                                                          2-843 4 NHCO NMe BnO                                                          2-844 4 NHCO NMe Z-1                                                          2-845 4 NHCO NMe Z-2                                                          2-846 4 NHCO NMe Z-3                                                          2-847 4 NHCO NMe Z-4                                                          2-848 4 NHCO NMe Z-5                                                          2-849 4 NHCO NMe Z-6                                                          2-850 4 NHCO NMe Z-7                                                          2-851 4 NHCO NMe Z-8                                                          2-852 4 NHCO NMe Z-9                                                          2-853 4 NHCO NMe Z-10                                                         2-854 4 NHCO NMe Z-11                                                         2-855 4 NHCO NMe Z-12                                                         2-856 4 NHCO NMe 3-Py                                                         2-857 4 NHCO NMe 4-Py                                                         2-858 4 NHCO NHNH H                                                           2-859 4 NHCO NHNH Me                                                          2-860 4 NHCO NHNH Et                                                          2-861 4 NHCO NHNH Me                                                          2-862 4 NHCO NHNH Et                                                          2-863 4 NHCO NHNH Pr                                                          2-864 4 NHCONHNHCO NH H                                                       2-865 4 NHCONHNHCO NH Ph                                                      2-866 4 NHCONHNHCO NH 2-Me-Ph                                                 2-867 4 NHCONHNHCO NH 4-Me-Ph                                                 2-868 4 NHCONHNHCO NH 2,4-diMe-Ph                                             2-869 4 NHCONHNHCO NH 3,4-diMe-Ph                                             2-870 4 NHCONHNHCO NH 2-(CF.sub.3)Ph                                          2-871 4 NHCONHNHCO NH 4-(CF.sub.3)Ph                                          2-872 4 NHCONHNHCO NH 2-MeOPh                                                 2-873 4 NHCONHNHCO NH 4-MeOPh                                                 2-874 4 NHCONHNHCO NH 2-EtOPh                                                 2-875 4 NHCONHNHCO NH 4-EtOPh                                                 2-876 4 NHCONHNHCO NH 2-HOPh                                                  2-877 4 NHCONHNHCO NH 4-HOPh                                                  2-878 4 NHCONHNHCO NH 2-(HOOC)Ph                                              2-879 4 NHCONHNHCO NH 4-(HOOC)Ph                                              2-880 4 NHCONHNHCO NH 2-(MeOOC)Ph                                             2-881 4 NHCONHNHCO NH 4-(MeOOC)Ph                                             2-882 4 NHCONHNHCO NH 2-(EtOOC)Ph                                             2-883 4 NHCONHNHCO NH 4-(EtOOC)Ph                                             2-884 4 NHCONHNHCO NH 2-(tBuOOC)Ph                                            2-885 4 NHCONHNHCO NH 4-(tBuOOC)Ph                                            2-886 4 NHCONHNHCO NH 2-Cl-Ph                                                 2-887 4 NHCONHNHCO NH 4-Cl-Ph                                                 2-888 4 NHCONHNHCO NH 2-Br-Ph                                                 2-889 4 NHCONHNHCO NH 4-Br-Ph                                                 2-890 4 NHCONHNHCO NH 2-I-Ph                                                  2-891 4 NHCONHNHCO NH 4-I-Ph                                                  2-892 4 NHCONHNHCO NH 2-NO.sub.2 -Ph                                          2-893 4 NHCONHNHCO NH 4-NO.sub.2 -Ph                                          2-894 4 NHCONHNHCO NH 2-NH.sub.2 -Ph                                          2-895 4 NHCONHNHCO NH 4-NH.sub.2 -Ph                                          2-896 4 NHCONHNHCO NH 2-(HO.sub.3 S)Ph                                        2-897 4 NHCONHNHCO NH 4-(HO.sub.3 S)Ph                                        2-898 4 NHCONHNHCO NH 2-(NH.sub.2 O.sub.2 S)Ph                                2-899 4 NHCONHNHCO NH 4-(NH.sub.2 O.sub.2 S)Ph                                2-900 4 NHCONHNHCO NH 2-CN-Ph                                                 2-901 4 NHCONHNHCO NH 4-CN-Ph                                                 2-902 4 NHCONHNHCO NH 2-(HOCH.sub.2)Ph                                        2-903 4 NHCONHNHCO NH 4-(HOCH.sub.2)Ph                                        2-904 4 NHCONHNHCO NH Me                                                      2-905 4 NHCONHNHCO NH Et                                                      2-906 4 NHCONHNHCO NH Pr                                                      2-907 4 NHCONHNHCO NH iPr                                                     2-908 4 NHCONHNHCO NH Bu                                                      2-909 4 NHCONHNHCO NH HOOCCH.sub.2 --                                         2-910 4 NHCONHNHCO NH MeOOCCH.sub.2 --                                        2-911 4 NHCONHNHCO NH MeCH(COOH)                                              2-912 4 NHCONHNHCO NH HOOC--(CH.sub.2).sub.2 --                               2-913 4 NHCONHNHCO NH MeCH(COOMe)                                             2-914 4 NHCONHNHCO NH 1-HOOC-iBu                                              2-915 4 NHCONHNHCO NH 1-MeOOC-iBu                                             2-916 4 NHCONHNHCO NH 1-HOOC-iPn                                              2-917 4 NHCONHNHCO NH 1-MeOOC-iPn                                             2-918 4 NHCONHNHCO NH 1-HOOC-2-Me-Bu                                          2-919 4 NHCONHNHCO NH 1-MeOOC-2-Me-Bu                                         2-920 4 NHCONHNHCO NH CH.sub.2 CH.sub.2 SO.sub.3 H                            2-921 4 NHCONHNHCO NH OH                                                      2-922 4 NHCONHNHCO NH MeO                                                     2-923 4 NHCONHNHCO NH EtO                                                     2-924 4 NHCONHNHCO NH PrO                                                     2-925 4 NHCONHNHCO NH iPrO                                                    2-926 4 NHCONHNHCO NH BuO                                                     2-927 4 NHCONHNHCO NH iBuO                                                    2-928 4 NHCONHNHCO NH sBuO                                                    2-929 4 NHCONHNHCO NH tBuO                                                    2-930 4 NHCONHNHCO NH HxO                                                     2-931 4 NHCONHNHCO NH PhO                                                     2-932 4 NHCONHNHCO NH BnO                                                     2-933 4 NHCONHNHCO NH Z-1                                                     2-934 4 NHCONHNHCO NH Z-2                                                     2-935 4 NHCONHNHCO NH Z-3                                                     2-936 4 NHCONHNHCO NH Z-4                                                     2-937 4 NHCONHNHCO NH Z-5                                                     2-938 4 NHCONHNHCO NH Z-6                                                     2-939 4 NHCONHNHCO NH Z-7                                                     2-940 4 NHCONHNHCO NH Z-8                                                     2-941 4 NHCONHNHCO NH Z-9                                                     2-942 4 NHCONHNHCO NH Z-10                                                    2-943 4 NHCONHNHCO NH Z-11                                                    2-944 4 NHCONHNHCO NH Z-12                                                    2-945 4 NHCONHNHCO NH 3-Py                                                    2-946 4 NHCONHNHCO NH 4-Py                                                    2-947 4 NHCONHCO -- H                                                         2-948 4 NHCONHCO -- Ph                                                        2-949 4 NHCONHCO -- 2-Me-Ph                                                   2-950 4 NHCONHCO -- 4-Me-Ph                                                   2-951 4 NHCONHCO -- 2,4-diMe-Ph                                               2-952 4 NHCONHCO -- 3,4-diMe-Ph                                               2-953 4 NHCONHCO -- 2-(CF.sub.3)Ph                                            2-954 4 NHCONHCO -- 4-(CF.sub.3)Ph                                            2-955 4 NHCONHCO -- 2-MeOPh                                                   2-956 4 NHCONHCO -- 4-MeOPh                                                   2-957 4 NHCONHCO -- 2-EtOPh                                                   2-958 4 NHCONHCO -- 4-EtOPh                                                   2-959 4 NHCONHCO -- 2-HOPh                                                    2-960 4 NHCONHCO -- 4-HOPh                                                    2-961 4 NHCONHCO -- 2-(HOOC)Ph                                                2-962 4 NHCONHCO -- 4-(HOOC)Ph                                                2-963 4 NHCONHCO -- 2-(MeOOC)Ph                                               2-964 4 NHCONHCO -- 4-(MeOOC)Ph                                               2-965 4 NHCONHCO -- 2-(EtOOC)Ph                                               2-966 4 NHCONHCO -- 4-(EtOOC)Ph                                               2-967 4 NHCONHCO -- 2-(tBuOOC)Ph                                              2-968 4 NHCONHCO -- 4-(tBuOOC)Ph                                              2-969 4 NHCONHCO -- 2-Cl-Ph                                                   2-970 4 NHCONHCO -- 4-Cl-Ph                                                   2-971 4 NHCONHCO -- 2-Br-Ph                                                   2-972 4 NHCONHCO -- 4-Br-Ph                                                   2-973 4 NHCONHCO -- 2-I-Ph                                                    2-974 4 NHCONHCO -- 4-I-Ph                                                    2-975 4 NHCONHCO -- 2-NO.sub.2 -Ph                                            2-976 4 NHCONHCO -- 4-NO.sub.2 -Ph                                            2-977 4 NHCONHCO -- 2-NH.sub.2 -Ph                                            2-978 4 NHCONHCO -- 4-NH.sub.2 -Ph                                            2-979 4 NHCONHCO -- 2-(HO.sub.3 S)Ph                                          2-980 4 NHCONHCO -- 4-(HO.sub.3 S)Ph                                          2-981 4 NHCONHCO -- 2-(NH.sub.2 O.sub.2 S)Ph                                  2-982 4 NHCONHCO -- 4-(NH.sub.2 O.sub.2 S)Ph                                  2-983 4 NHCONHCO -- 2-CN-Ph                                                   2-984 4 NHCONHCO -- 4-CN-Ph                                                   2-985 4 NHCONHCO -- 2-(HOCH.sub.2)Ph                                          2-986 4 NHCONHCO -- 4-(HOCH.sub.2)Ph                                          2-987 4 NHCONHCO -- Me                                                        2-988 4 NHCONHCO -- Et                                                        2-989 4 NHCONHCO -- Pr                                                        2-990 4 NHCONHCO -- iPr                                                       2-991 4 NHCONHCO -- Bu                                                        2-992 4 NHCONHCO -- HOOCCH.sub.2 --                                           2-993 4 NHCONHCO -- MeOOCCH.sub.2 --                                          2-994 4 NHCONHCO -- MeCH(COOH)                                                2-995 4 NHCONHCO -- HOOC--(CH.sub.2).sub.2 --                                 2-996 4 NHCONHCO -- MeCH(COOMe)                                               2-997 4 NHCONHCO -- 1-HOOC-iBu                                                2-998 4 NHCONHCO -- 1-MeOOC-iBu                                               2-999 4 NHCONHCO -- 1-HOOC-iPn                                                2-1000 4 NHCONHCO -- 1-MeOOC-iPn                                              2-1001 4 NHCONHCO -- 1-HOOC-2-Me-Bu                                           2-1002 4 NHCONHCO -- 1-MeOOC-2-Me-Bu                                          2-1003 4 NHCONHCO -- CH.sub.2 CH.sub.2 SO.sub.3 H                             2-1004 4 NHCONHCO -- MeO                                                      2-1005 4 NHCONHCO -- EtO                                                      2-1006 4 NHCONHCO -- PrO                                                      2-1007 4 NHCONHCO -- iPrO                                                     2-1008 4 NHCONHCO -- BuO                                                      2-1009 4 NHCONHCO -- iBuO                                                     2-1010 4 NHCONHCO -- sBuO                                                     2-1011 4 NHCONHCO -- tBuO                                                     2-1012 4 NHCONHCO -- HxO                                                      2-1013 4 NHCONHCO -- PhO                                                      2-1014 4 NHCONHCO -- BnO                                                      2-1015 4 NHCONHCO -- Z-1                                                      2-1016 4 NHCONHCO -- Z-2                                                      2-1017 4 NHCONHCO -- Z-3                                                      2-1018 4 NHCONHCO -- Z-4                                                      2-1019 4 NHCONHCO -- Z-5                                                      2-1020 4 NHCONHCO -- Z-6                                                      2-1021 4 NHCONHCO -- Z-7                                                      2-1022 4 NHCONHCO -- Z-8                                                      2-1023 4 NHCONHCO -- Z-9                                                      2-1024 4 NHCONHCO -- Z-10                                                     2-1025 4 NHCONHCO -- Z-11                                                     2-1026 4 NHCONHCO -- Z-12                                                     2-1027 4 NHCONHCO -- 3-Py                                                     2-1028 4 NHCONHCO -- 4-Py                                                     2-1029 4 NHCONHSO.sub.2 -- H                                                  2-1030 4 NHCONHSO.sub.2 -- Ph                                                 2-1031 4 NHCONHSO.sub.2 -- 2-Me-Ph                                            2-1032 4 NHCONHSO.sub.2 -- 4-Me-Ph                                            2-1033 4 NHCONHSO.sub.2 -- 2,4-diMe-Ph                                        2-1034 4 NHCONHSO.sub.2 -- 3,4-diMe-Ph                                        2-1035 4 NHCONHSO.sub.2 -- 2-(CF.sub.3)Ph                                     2-1036 4 NHCONHSO.sub.2 -- 4-(CF.sub.3)Ph                                     2-1037 4 NHCONHSO.sub.2 -- 2-MeOPh                                            2-1038 4 NHCONHSO.sub.2 -- 4-MeOPh                                            2-1039 4 NHCONHSO.sub.2 -- 2-EtOPh                                            2-1040 4 NHCONHSO.sub.2 -- 4-EtOPh                                            2-1041 4 NHCONHSO.sub.2 -- 2-HOPh                                             2-1042 4 NHCONHSO.sub.2 -- 4-HOPh                                             2-1043 4 NHCONHSO.sub.2 -- 2-(HOOC)Ph                                         2-1044 4 NHCONHSO.sub.2 -- 4-(HOOC)Ph                                         2-1045 4 NHCONHSO.sub.2 -- 2-(MeOOC)Ph                                        2-1046 4 NHCONHSO.sub.2 -- 4-(MeOOC)Ph                                        2-1047 4 NHCONHSO.sub.2 -- 2-(EtOOC)Ph                                        2-1048 4 NHCONHSO.sub.2 -- 4-(EtOOC)Ph                                        2-1049 4 NHCONHSO.sub.2 -- 2-(tBuOOC)Ph                                       2-1050 4 NHCONHSO.sub.2 -- 4-(tBuOOC)Ph                                       2-1051 4 NHCONHSO.sub.2 -- 2-Cl-Ph                                            2-1052 4 NHCONHSO.sub.2 -- 4-Cl-Ph                                            2-1053 4 NHCONHSO.sub.2 -- 2-Br-Ph                                            2-1054 4 NHCONHSO.sub.2 -- 4-Br-Ph                                            2-1055 4 NHCONHSO.sub.2 -- 2-I-Ph                                             2-1056 4 NHCONHSO.sub.2 -- 4-I-Ph                                             2-1057 4 NHCONHSO.sub.2 -- 2-NO.sub.2 -Ph                                     2-1058 4 NHCONHSO.sub.2 -- 4-NO.sub.2 -Ph                                     2-1059 4 NHCONHSO.sub.2 -- 2-NH.sub.2 -Ph                                     2-1060 4 NHCONHSO.sub.2 -- 4-NH.sub.2 -Ph                                     2-1061 4 NHCONHSO.sub.2 -- 2-(HO.sub.3 S)Ph                                   2-1062 4 NHCONHSO.sub.2 -- 4-(HO.sub.3 S)Ph                                   2-1063 4 NHCONHSO.sub.2 -- 2-(NH.sub.2 O.sub.2 S)Ph                           2-1064 4 NHCONHSO.sub.2 -- 4-(NH.sub.2 O.sub.2 S)Ph                           2-1065 4 NHCONHSO.sub.2 -- 2-CN-Ph                                            2-1066 4 NHCONHSO.sub.2 -- 4-CN-Ph                                            2-1067 4 NHCONHSO.sub.2 -- 2-(HOCH.sub.2)Ph                                   2-1068 4 NHCONHSO.sub.2 -- 4-(HOCH.sub.2)Ph                                   2-1069 4 NHCONHSO.sub.2 -- Me                                                 2-1070 4 NHCONHSO.sub.2 -- Et                                                 2-1071 4 NHCONHSO.sub.2 -- Pr                                                 2-1072 4 NHCONHSO.sub.2 -- iPr                                                2-1073 4 NHCONHSO.sub.2 -- Bu                                                 2-1074 4 NHCONHSO.sub.2 -- HOOCCH.sub.2 --                                    2-1075 4 NHCONHSO.sub.2 -- MeOOCCH.sub.2 --                                   2-1076 4 NHCONHSO.sub.2 -- MeCH(COOH)                                         2-1077 4 NHCONHSO.sub.2 -- HOOC--(CH.sub.2).sub.2 --                          2-1078 4 NHCONHSO.sub.2 -- MeCH(COOMe)                                        2-1079 4 NHCONHSO.sub.2 -- 1-HOOC-iBu                                         2-1080 4 NHCONHSO.sub.2 -- 1-MeOOC-iBu                                        2-1081 4 NHCONHSO.sub.2 -- 1-HOOC-iPn                                         2-1082 4 NHCONHSO.sub.2 -- 1-MeOOC-iPn                                        2-1083 4 NHCONHSO.sub.2 -- 1-HOOC-2-Me-Bu                                     2-1084 4 NHCONHSO.sub.2 -- 1-MeOOC-2-Me-Bu                                    2-1085 4 NHCONHSO.sub.2 -- CH.sub.2 CH.sub.2 SO.sub.3 H                       2-1086 4 NHCONHSO.sub.2 -- OH                                                 2-1087 4 NHCONHSO.sub.2 -- MeO                                                2-1088 4 NHCONHSO.sub.2 -- EtO                                                2-1089 4 NHCONHSO.sub.2 -- PrO                                                2-1090 4 NHCONHSO.sub.2 -- iPrO                                               2-1091 4 NHCONHSO.sub.2 -- BuO                                                2-1092 4 NHCONHSO.sub.2 -- iBuO                                               2-1093 4 NHCONHSO.sub.2 -- sBuO                                               2-1094 4 NHCONHSO.sub.2 -- tBuO                                               2-1095 4 NHCONHSO.sub.2 -- HxO                                                2-1096 4 NHCONHSO.sub.2 -- PhO                                                2-1097 4 NHCONHSO.sub.2 -- BnO                                                2-1098 4 NHCONHSO.sub.2 -- Z-1                                                2-1099 4 NHCONHSO.sub.2 -- Z-2                                                2-1100 4 NHCONHSO.sub.2 -- Z-3                                                2-1101 4 NHCONHSO.sub.2 -- Z-4                                                2-1102 4 NHCONHSO.sub.2 -- Z-5                                                2-1103 4 NHCONHSO.sub.2 -- Z-6                                                2-1104 4 NHCONHSO.sub.2 -- Z-7                                                2-1105 4 NHCONHSO.sub.2 -- Z-8                                                2-1106 4 NHCONHSO.sub.2 -- Z-9                                                2-1107 4 NHCONHSO.sub.2 -- Z-10                                               2-1108 4 NHCONHSO.sub.2 -- Z-11                                               2-1109 4 NHCONHSO.sub.2 -- Z-12                                               2-1110 4 NHCONHSO.sub.2 -- 3-Py                                               2-1111 4 NHCONHSO.sub.2 -- 4-Py                                               2-1112 4 NHCONHSO.sub.2 NH H                                                  2-1113 4 NHCONHSO.sub.2 NH Me                                                 2-1114 4 NHCONHSO.sub.2 NH Et                                                 2-1115 4 NHCONHSO.sub.2 NH Pr                                                 2-1116 4 NHCONHSO.sub.2 NH iPr                                                2-1117 4 NHCONHSO.sub.2 NH Bu                                                 2-1118 4 NHCONHSO.sub.2 NMe Me                                                2-1119 4 NHCONHSO.sub.2 NMe Et                                                2-1120 4 NHCONHSO.sub.2 NMe Pr                                                2-1121 4 NHCONHSO.sub.2 NMe iPr                                               2-1122 4 NHCONHSO.sub.2 NMe Bu                                                2-1123 4 -- NH H                                                              2-1124 4 -- NH Me                                                             2-1125 4 -- NH Et                                                             2-1126 4 -- NH Pr                                                             2-1127 4 -- NH iPr                                                            2-1128 4 -- NH Bu                                                           2-1129                                                                              4     CO            Pyr                                                   2-1130 4 CO Pipri                                                             2-1131 4 CO Pipra                                                             2-1132 4 CO Mor                                                               2-1133 4 CO Thmor                                                             2-1134 4 CO NHPyr                                                             2-1135 4 CO NHPipri                                                           2-1136 4 CO NHPipra                                                           2-1137 4 CO NHMor                                                             2-1138 4 CO NHThmor                                                           2-1139 4 NHCO Pyr                                                             2-1140 4 NHCO Pipri                                                           2-1141 4 NHCO Pipra                                                           2-1142 4 NHCO Mor                                                             2-1143 4 NHCO Thmor                                                           2-1144 4 NHCO NHPyr                                                           2-1145 4 NHCO NHPipri                                                         2-1146 4 NHCO NHPipra                                                         2-1147 4 NHCO NHMor                                                           2-1148 4 NHCO NHThmor                                                         2-1149 4 CONHCO Pyr                                                           2-1150 4 CONHCO Pipri                                                         2-1151 4 CONHCO Pipra                                                         2-1152 4 CONHCO Mor                                                           2-1153 4 CONHCO Thmor                                                         2-1154 4 CONHCO NHPyr                                                         2-1155 4 CONHCO NHPipri                                                       2-1156 4 CONHCO NHPipra                                                       2-1157 4 CONHCO NHMor                                                         2-1158 4 CONHCO NHThmor                                                       2-1159 4 CONHSO.sub.2 Pyr                                                     2-1160 4 CONHSO.sub.2 Pipri                                                   2-1161 4 CONHSO.sub.2 Pipra                                                   2-1162 4 CONHSO.sub.2 Mor                                                     2-1163 4 CONHSO.sub.2 Thmor                                                   2-1164 4 CONHSO.sub.2 NHPyr                                                   2-1165 4 CONHSO.sub.2 NHPipri                                                 2-1166 4 CONHSO.sub.2 NHPipra                                                 2-1167 4 CONHSO.sub.2 NHMor                                                   2-1168 4 CONHSO.sub.2 NHThmor                                               2-1169                                                                              4     NHSO.sub.2    NH    Z-4                                             2-1170 4 NHSO.sub.2 -- Me                                                     2-1171 4 NHSO.sub.2 -- Et                                                     2-1172 4 NHSO.sub.2 -- Pr                                                     2-1173 4 NHSO.sub.2 -- CH.sub.2 --Cl                                          2-1174 4 NHSO.sub.2 -- Ph                                                     2-1175 4 NHSO.sub.2 -- 4-Me-Ph                                                2-1176 4 CO NMe Ph                                                            2-1177 4 CO NMe 2-Me-Ph                                                       2-1178 4 CO NMe 4-Me-Ph                                                       2-1179 4 CO NMe 2,4-diMe-Ph                                                   2-1180 4 CO NMe 3,4-diMe-Ph                                                   2-1181 4 CO NMe 2-(CF.sub.3)Ph                                                2-1182 4 CO NMe 4-(CF.sub.3)Ph                                                2-1183 4 CO NMe 2-MeOPh                                                       2-1184 4 CO NMe 4-MeOPh                                                       2-1185 4 CO NMe 2-EtOPh                                                       2-1186 4 CO NMe 4-EtOPh                                                       2-1187 4 CO NMe 2-HOPh                                                        2-1188 4 CO NMe 4-HOPh                                                        2-1189 4 CO NMe 2-(HOOC)Ph                                                    2-1190 4 CO NMe 4-(HOOC)Ph                                                    2-1191 4 CO NMe 2-(MeOOC)Ph                                                   2-1192 4 CO NMe 4-(MeOOC)Ph                                                   2-1193 4 CO NMe 2-(EtOOC)Ph                                                   2-1194 4 CO NMe 4-(EtOOC)Ph                                                   2-1195 4 CO NMe 2-(tBuOOC)Ph                                                  2-1196 4 CO NMe 4-(tBuOOC)Ph                                                  2-1197 4 CO NMe 2-Cl-Ph                                                       2-1198 4 CO NMe 4-Cl-Ph                                                       2-1199 4 CO NMe 2-Br-Ph                                                       2-1200 4 CO NMe 4-Br-Ph                                                       2-1201 4 CO NMe 2-I-Ph                                                        2-1202 4 CO NMe 4-I-Ph                                                        2-1203 4 CO NMe 2-NO.sub.2 -Ph                                                2-1204 4 CO NMe 4-NO.sub.2 -Ph                                                2-1205 4 CO NMe 2-NH.sub.2 -Ph                                                2-1206 4 CO NMe 4-NH.sub.2 -Ph                                                2-1207 4 CO NMe 2-(HO.sub.3 S)Ph                                              2-1208 4 CO NMe 4-(HO.sub.3 S)Ph                                              2-1209 4 CO NMe 2-(NH.sub.2 O.sub.2 S)Ph                                      2-1210 4 CO NMe 4-(NH.sub.2 O.sub.2 S)Ph                                      2-1211 4 CO NMe 2-CN-Ph                                                       2-1212 4 CO NMe 4-CN-Ph                                                       2-1213 4 CO NMe 2-(HOCH.sub.2)Ph                                              2-1214 4 CO NMe 4-(HOCH.sub.2)Ph                                              2-1215 4 CO NMe Me                                                            2-1216 4 CO NMe Et                                                            2-1217 4 CO NMe Pr                                                            2-1218 4 CO NMe iPr                                                           2-1219 4 CO NMe Bu                                                            2-1220 4 CO NMe HOOCCH.sub.2 --                                               2-1221 4 CO NMe MeOOCCH.sub.2 --                                              2-1222 4 CO NMe MeCH(COOH)                                                    2-1223 4 CO NMe HOOC--(CH.sub.2).sub.2 --                                     2-1224 4 CO NMe MeCH(COOMe)                                                   2-1225 4 CO NMe 1-HOOC-iBu                                                    2-1226 4 CO NMe 1-MeOOC-iBu                                                   2-1227 4 CO NMe 1-HOOC-iPn                                                    2-1228 4 CO NMe 1-MeOOC-iPn                                                   2-1229 4 CO NMe 1-HOOC-2-Me-Bu                                                2-1230 4 CO NMe 1-MeOOC-2-Me-Bu                                               2-1231 4 CO NMe CH.sub.2 CH.sub.2 SO.sub.3 H                                  2-1232 4 CO NMe OH                                                            2-1233 4 CO NMe MeO                                                           2-1234 4 CO NMe EtO                                                           2-1235 4 CO NMe PrO                                                           2-1236 4 CO NMe iPrO                                                          2-1237 4 CO NMe BuO                                                           2-1238 4 CO NMe iBuO                                                          2-1239 4 CO NMe sBuO                                                          2-1240 4 CO NMe tBuO                                                          2-1241 4 CO NMe HxO                                                           2-1242 4 CO NMe PhO                                                           2-1243 4 CO NMe BnO                                                           2-1244 4 CO NMe Z-1                                                           2-1245 4 CO NMe Z-2                                                           2-1246 4 CO NMe Z-3                                                           2-1247 4 CO NMe Z-4                                                           2-1248 4 CO NMe Z-5                                                           2-1249 4 CO NMe Z-6                                                           2-1250 4 CO NMe Z-7                                                           2-1251 4 CO NMe Z-8                                                           2-1252 4 CO NMe Z-9                                                           2-1253 4 CO NMe Z-10                                                          2-1254 4 CO NMe Z-11                                                          2-1255 4 CO NMe Z-12                                                          2-1256 4 CO NMe 3-Py                                                          2-1257 4 CO NMe 4-Py                                                        2-1258                                                                              4     CO            Thiad                                                 2-1259 4 CO NHThiad                                                           2-1260 4 NHCO Thiad                                                           2-1261 4 NHCO NHThiad                                                         2-1262 4 CONHCO Thiad                                                         2-1263 4 CONHCO NHThiad                                                       2-1264 4 CONHSO.sub.2 Thiad                                                   2-1265 4 CONHSO.sub.2 NHThiad                                               2-1266                                                                              4     NHCS          NH    H                                               2-1267 4 NHCS NH Me                                                           2-1268 4 NHCS NH Et                                                           2-1269 4 NHCS NH Ph                                                           2-1270 4 NHCS NH HOOCCH.sub.2 --                                              2-1271 4 NHCS NH MeOOCCH.sub.2 --                                             2-1272 4 NHCS NH MeCH(COOH)                                                   2-1273 4 NHCS NH HOOC--(CH.sub.2).sub.2 --                                    2-1274 4 NHCS NH MeCH(COOMe)                                                  2-1275 4 CO NH HOOC--(CH.sub.2).sub.3 --                                      2-1276 4 NHCO NH HOOC--(CH.sub.2).sub.3 --                                    2-1277 4 NHCO -- HOOC--(CH.sub.2).sub.3 --                                    2-1278 4 NHCS NH HOOC--(CH.sub.2).sub.3 --                                    2-1279 4 CO NH MeSO.sub.2 NHCOCH(Me)                                          2-1280 4 NHCO NH MeSO.sub.2 NHCOCH(Me)                                        2-1281 4 NHCO -- MeSO.sub.2 NHCOCH(Me)                                        2-1282 4 NHCS NH MeSO.sub.2 NHCOCH(Me)                                        2-1283 4 -- NH HOOCCH.sub.2 --                                                2-1284 4 -- NH MeOOCCH.sub.2 --                                               2-1285 4 -- NH MeCH(COOH)                                                     2-1286 4 -- NH HOOC--(CH.sub.2).sub.2 --                                      2-1287 4 -- NH MeCH(COOMe)                                                    2-1288 4 -- NH HOOC--(CH.sub.2).sub.3 --                                      2-1289 4 NHCOCO -- OH                                                         2-1290 4 NHCOCO -- MeO                                                        2-1291 4 NHCOCO -- EtO                                                        2-1292 4 NHCOCO -- PrO                                                        2-1293 4 NHCOCO -- iPrO                                                       2-1294 4 NHCOCO -- BuO                                                        2-1295 4 NHCOCO -- iBuO                                                       2-1296 4 NHCOCO -- sBuO                                                       2-1297 4 NHCOCO -- tBuO                                                       2-1298 4 NHCOCO -- HxO                                                        2-1299 4 NHCOCO -- PhO                                                        2-1300 4 NHCOCO -- BnO                                                        2-1301 5 CO NH H                                                              2-1302 5 CO NH Ph                                                             2-1303 5 CO NH 2-Me-Ph                                                        2-1304 5 CO NH 4-Me-Ph                                                        2-1305 5 CO NH 2,4-diMe-Ph                                                    2-1306 5 CO NH 3,4-diMe-Ph                                                    2-1307 5 CO NH 2-(CF.sub.3)Ph                                                 2-1308 5 CO NH 4-(CF.sub.3)Ph                                                 2-1309 5 CO NH 2-MeOPh                                                        2-1310 5 CO NH 4-MeOPh                                                        2-1311 5 CO NH 2-EtOPh                                                        2-1312 5 CO NH 4-EtOPh                                                        2-1313 5 CO NH 2-HOPh                                                         2-1314 5 CO NH 4-HOPh                                                         2-1315 5 CO NH 2-(HOOC)Ph                                                     2-1316 5 CO NH 4-(HOOC)Ph                                                     2-1317 5 CO NH 2-(MeOOC)Ph                                                    2-1318 5 CO NH 4-(MeOOC)Ph                                                    2-1319 5 CO NH 2-(EtOOC)Ph                                                    2-1320 5 CO NH 4-(EtOOC)Ph                                                    2-1321 5 CO NH 2-(tBuOOC)Ph                                                   2-1322 5 CO NH 4-(tBuOOC)Ph                                                   2-1323 5 CO NH 2-Cl-Ph                                                        2-1324 5 CO NH 4-Cl-Ph                                                        2-1325 5 CO NH 2-Br-Ph                                                        2-1326 5 CO NH 4-Br-Ph                                                        2-1327 5 CO NH 2-I-Ph                                                         2-1328 5 CO NH 4-I-Ph                                                         2-1329 5 CO NH 2-NO.sub.2 -Ph                                                 2-1330 5 CO NH 4-NO.sub.2 -Ph                                                 2-1331 5 CO NH 2-NH.sub.2 -Ph                                                 2-1332 5 CO NH 4-NH.sub.2 -Ph                                                 2-1333 5 CO NH 2-(HO.sub.3 S)Ph                                               2-1334 5 CO NH 4-(HO.sub.3 S)Ph                                               2-1335 5 CO NH 2-(NH.sub.2 O.sub.2 S)Ph                                       2-1336 5 CO NH 4-(NH.sub.2 O.sub.2 S)Ph                                       2-1337 5 CO NH 2-CN-Ph                                                        2-1338 5 CO NH 4-CN-Ph                                                        2-1339 5 CO NH 2-(HOCH.sub.2)Ph                                               2-1340 5 CO NH 4-(HOCH.sub.2)Ph                                               2-1341 5 CO NH Me                                                             2-1342 5 CO NH Et                                                             2-1343 5 CO NH Pr                                                             2-1344 5 CO NH iPr                                                            2-1345 5 CO NH Bu                                                             2-1346 5 CO NH HOOCCH.sub.2 --                                                2-1347 5 CO NH MeOOCCH.sub.2 --                                               2-1348 5 CO NH MeCH(COOH)                                                     2-1349 5 CO NH HOOC--(CH.sub.2).sub.2 --                                      2-1350 5 CO NH MeCH(COOMe)                                                    2-1351 5 CO NH 1-HOOC-iBu                                                     2-1352 5 CO NH 1-MeOOC-iBu                                                    2-1353 5 CO NH 1-HOOC-iPn                                                     2-1354 5 CO NH 1-MeOOC-iPn                                                    2-1355 5 CO NH 1-HOOC-2-Me-Bu                                                 2-1356 5 CO NH 1-MeOOC-2-Me-Bu                                                2-1357 5 CO NH CH.sub.2 CH.sub.2 SO.sub.2 H                                   2-1358 5 CO NH OH                                                             2-1359 5 CO NH MeO                                                            2-1360 5 CO NH EtO                                                            2-1361 5 CO NH PrO                                                            2-1362 5 CO NH iPrO                                                           2-1363 5 CO NH BuO                                                            2-1364 5 CO NH iBuO                                                           2-1365 5 CO NH sBuO                                                           2-1366 5 CO NH tBuO                                                           2-1367 5 CO NH HxO                                                            2-1368 5 CO NH PhO                                                            2-1369 5 CO NH BnO                                                            2-1370 5 CO NH Z-1                                                            2-1371 5 CO NH Z-2                                                            2-1372 5 CO NH Z-3                                                            2-1373 5 CO NH Z-4                                                            2-1374 5 CO NH Z-5                                                            2-1375 5 CO NH Z-6                                                            2-1376 5 CO NH Z-7                                                            2-1377 5 CO NH Z-8                                                            2-1378 5 CO NH Z-9                                                            2-1379 5 CO NH Z-10                                                           2-1380 5 CO NH Z-11                                                           2-1381 5 CO NH Z-12                                                           2-1382 5 CO NH 3-Py                                                           2-1383 5 CO NH 4-Py                                                           2-1384 5 CO N(Ac) H                                                           2-1385 5 CO N(Ac) Ph                                                          2-1386 5 CO N(Ac) 2-Me-Ph                                                     2-1387 5 CO N(Ac) 4-Me-Ph                                                     2-1388 5 CO N(Ac) 2,4-diMe-Ph                                                 2-1389 5 CO N(Ac) 3,4-diMe-Ph                                                 2-1390 5 CO N(Ac) 2-(CF.sub.3)Ph                                              2-1391 5 CO N(Ac) 4-(CF.sub.3)Ph                                              2-1392 5 CO N(Ac) 2-MeOPh                                                     2-1393 5 CO N(Ac) 4-MeOPh                                                     2-1394 5 CO N(Ac) 2-EtOPh                                                     2-1395 5 CO N(Ac) 4-EtOPh                                                     2-1396 5 CO N(Ac) 2-HOPh                                                      2-1397 5 CO N(Ac) 4-HOPh                                                      2-1398 5 CO N(Ac) 2-(HOOC)Ph                                                  2-1399 5 CO N(Ac) 4-(HOOC)Ph                                                  2-1400 5 CO N(Ac) 2-(MeOOC)Ph                                                 2-1401 5 CO N(Ac) 4-(MeOOC)Ph                                                 2-1402 5 CO N(Ac) 2-(EtOOC)Ph                                                 2-1403 5 CO N(Ac) 4-(EtOOC)Ph                                                 2-1404 5 CO N(Ac) 2-(tBuOOC)Ph                                                2-1405 5 CO N(Ac) 4-(tBuOOC)Ph                                                2-1406 5 CO N(Ac) 2-Cl-Ph                                                     2-1407 5 CO N(Ac) 4-Cl-Ph                                                     2-1408 5 CO N(Ac) 2-Br-Ph                                                     2-1409 5 CO N(Ac) 4-Br-Ph                                                     2-1410 5 CO N(Ac) 2-I-Ph                                                      2-1411 5 CO N(Ac) 4-I-Ph                                                      2-1412 5 CO N(Ac) 2-NO.sub.2 -Ph                                              2-1413 5 CO N(Ac) 4-NO.sub.2 -Ph                                              2-1414 5 CO N(Ac) 2-NH.sub.2 -Ph                                              2-1415 5 CO N(Ac) 4-NH.sub.2 -Ph                                              2-1416 5 CO N(Ac) 2-(HO.sub.3 S)Ph                                            2-1417 5 CO N(Ac) 4-(HO.sub.3 S)Ph                                            2-1418 5 CO N(Ac) 2-(NH.sub.2 O.sub.2 S)Ph                                    2-1419 5 CO N(Ac) 4-(NH.sub.2 O.sub.2 S)Ph                                    2-1420 5 CO N(Ac) 2-CN-Ph                                                     2-1421 5 CO N(Ac) 4-CN-Ph                                                     2-1422 5 CO N(Ac) 2-(HOCH.sub.2)Ph                                            2-1423 5 CO N(Ac) 4-(HOCH.sub.2)Ph                                            2-1424 5 CO N(Ac) Me                                                          2-1425 5 CO N(Ac) Et                                                          2-1426 5 CO N(Ac) Pr                                                          2-1427 5 CO N(Ac) iPr                                                         2-1428 5 CO N(Ac) Bu                                                          2-1429 5 CO N(Ac) HOOCCH.sub.2 --                                             2-1430 5 CO N(Ac) MeOOCCH.sub.2 --                                            2-1431 5 CO N(Ac) MeCH(COOH)                                                  2-1432 5 CO N(Ac) HOOC--(CH.sub.2).sub.2 --                                   2-1433 5 CO N(Ac) MeCH-(COOMe)                                                2-1434 5 CO N(Ac) 1-HOOC-iBu                                                  2-1435 5 CO N(Ac) 1-MeOOC-iBu                                                 2-1436 5 CO N(Ac) 1-HOOC-iPn                                                  2-1437 5 CO N(Ac) 1-MeOOC-iPn                                                 2-1438 5 CO N(Ac) 1-HOOC-2-Me-Bu                                              2-1439 5 CO N(Ac) 1-MeOOC-2-Me-Bu                                             2-1440 5 CO N(Ac) CH.sub.2 CH.sub.2 SO.sub.3 H                                2-1441 5 CO N(Ac) OH                                                          2-1442 5 CO N(Ac) MeO                                                         2-1443 5 CO N(Ac) EtO                                                         2-1444 5 CO N(Ac) PrO                                                         2-1445 5 CO N(Ac) iPrO                                                        2-1446 5 CO N(Ac) BuO                                                         2-1447 5 CO N(Ac) iBuO                                                        2-1448 5 CO N(Ac) sBuO                                                        2-1449 5 CO N(Ac) tBuO                                                        2-1450 5 CO N(Ac) HxO                                                         2-1451 5 CO N(Ac) PhO                                                         2-1452 5 CO N(Ac) BnO                                                         2-1453 5 CO N(Ac) Z-1                                                         2-1454 5 CO N(Ac) Z-2                                                         2-1455 5 CO N(Ac) Z-3                                                         2-1456 5 CO N(Ac) Z-4                                                         2-1457 5 CO N(Ac) Z-5                                                         2-1458 5 CO N(Ac) Z-6                                                         2-1459 5 CO N(Ac) Z-7                                                         2-1460 5 CO N(Ac) Z-8                                                         2-1461 5 CO N(Ac) Z-9                                                         2-1462 5 CO N(Ac) Z-10                                                        2-1463 5 CO N(Ac) Z-11                                                        2-1464 5 CO N(Ac) Z-12                                                        2-1465 5 CO N(Ac) 3-Py                                                        2-1466 5 CO N(Ac) 4-Py                                                        2-1467 5 COO -- H                                                             2-1468 5 COO -- Ph                                                            2-1469 5 COO -- 2-Me-Ph                                                       2-1470 5 COO -- 4-Me-Ph                                                       2-1471 5 COO -- 2,4-diMe-Ph                                                   2-1472 5 COO -- 3,4-diMe-Ph                                                   2-1473 5 COO -- 2-(CF.sub.3)Ph                                                2-1474 5 COO -- 4-(CF.sub.3)Ph                                                2-1475 5 COO -- 2-MeOPh                                                       2-1476 5 COO -- 4-MeOPh                                                       2-1477 5 COO -- 2-EtOPh                                                       2-1478 5 COO -- 4-EtOPh                                                       2-1479 5 COO -- 2-HOPh                                                        2-1480 5 COO -- 4-HOPh                                                        2-1481 5 COO -- 2-(HOOC)Ph                                                    2-1482 5 COO -- 4-(HOOC)Ph                                                    2-1483 5 COO -- 2-(MeOOC)Ph                                                   2-1484 5 COO -- 4-(MeOOC)Ph                                                   2-1485 5 COO -- 2-(EtOOC)Ph                                                   2-1486 5 COO -- 4-(EtOOC)Ph                                                   2-1487 5 COO -- 2-(tBuOOC)Ph                                                  2-1488 5 COO -- 4-(tBuOOC)Ph                                                  2-1489 5 COO -- 2-Cl-Ph                                                       2-1490 5 COO -- 4-Cl-Ph                                                       2-1491 5 COO -- 2-Br-Ph                                                       2-1492 5 COO -- 4-Br-Ph                                                       2-1493 5 COO -- 2-I-Ph                                                        2-1494 5 COO -- 4-I-Ph                                                        2-1495 5 COO -- 2-NO.sub.2 -Ph                                                2-1496 5 COO -- 4-NO.sub.2 -Ph                                                2-1497 5 COO -- 2-NH.sub.2 -Ph                                                2-1498 5 COO -- 4-NH.sub.2 -Ph                                                2-1499 5 COO -- 2-(HO.sub.3 S)Ph                                              2-1500 5 COO -- 4-(HO.sub.3 S)Ph                                              2-1501 5 COO -- 2-(NH.sub.2 O.sub.2 S)Ph                                      2-1502 5 COO -- 4-(NH.sub.2 O.sub.2 S)Ph                                      2-1503 5 COO -- 2-CN-Ph                                                       2-1504 5 COO -- 4-CN-Ph                                                       2-1505 5 COO -- 2-(HOCH.sub.2)Ph                                              2-1506 5 COO -- 4-(HOCH.sub.2)Ph                                              2-1507 5 COO -- Me                                                            2-1508 5 COO -- Et                                                            2-1509 5 COO -- Pr                                                            2-1510 5 COO -- iPr                                                           2-1511 5 COO -- Bu                                                            2-1512 5 COO -- HOOCCH.sub.2 --                                               2-1513 5 COO -- HOOC--(CH.sub.2).sub.2 --                                     2-1514 5 COO -- MeCH(COOMe)                                                   2-1515 5 COO -- 1-HOOC-iBu                                                    2-1516 5 COO -- 1-HOOC-iPn                                                    2-1517 5 COO -- Z-1                                                           2-1518 5 COO -- Z-2                                                           2-1519 5 COO -- Z-3                                                           2-1520 5 COO -- Z-4                                                           2-1521 5 COO -- Z-5                                                           2-1522 5 COO -- Z-6                                                           2-1523 5 COO -- Z-7                                                           2-1524 5 COO -- Z-8                                                           2-1525 5 COO -- Z-9                                                           2-1526 5 COO -- Z-10                                                          2-1527 5 COO -- Z-11                                                          2-1528 5 COO -- Z-12                                                          2-1529 5 COO -- 3-Py                                                          2-1530 5 COO -- 4-Py                                                          2-1531 5 CONHCO -- H                                                          2-1532 5 CONHCO -- Ph                                                         2-1533 5 CONHCO -- 2-Me-Ph                                                    2-1534 5 CONHCO -- 4-Me-Ph                                                    2-1535 5 CONHCO -- 2,4-diMe-Ph                                                2-1536 5 CONHCO -- 3,4-diMe-Ph                                                2-1537 5 CONHCO -- 2-(CF.sub.3)Ph                                             2-1538 5 CONHCO -- 4-(CF.sub.3)Ph                                             2-1539 5 CONHCO -- 2-MeOPh                                                    2-1540 5 CONHCO -- 4-MeOPh                                                    2-1541 5 CONHCO -- 2-EtOPh                                                    2-1542 5 CONHCO -- 4-EtOPh                                                    2-1543 5 CONHCO -- 2-HOPh                                                     2-1544 5 CONHCO -- 4-HOPh                                                     2-1545 5 CONHCO -- 2-(HOOC)Ph                                                 2-1546 5 CONHCO -- 4-(HOOC)Ph                                                 2-1547 5 CONHCO -- 2-(MeOOC)Ph                                                2-1548 5 CONHCO -- 4-(MeOOC)Ph                                                2-1549 5 CONHCO -- 2-(EtOOC)Ph                                                2-1550 5 CONHCO -- 4-(EtOOC)Ph                                                2-1551 5 CONHCO -- 2-(tBuOOC)Ph                                               2-1552 5 CONHCO -- 4-(tBuOOC)Ph                                               2-1553 5 CONHCO -- 2-Cl-Ph                                                    2-1554 5 CONHCO -- 4-Cl-Ph                                                    2-1555 5 CONHCO -- 2-Br-Ph                                                    2-1556 5 CONHCO -- 4-Br-Ph                                                    2-1557 5 CONHCO -- 2-I-Ph                                                     2-1558 5 CONHCO -- 4-I-Ph                                                     2-1559 5 CONHCO -- 2-NO.sub.2 -Ph                                             2-1560 5 CONHCO -- 4-NO.sub.2 -Ph                                             2-1561 5 CONHCO -- 2-NH.sub.2 -Ph                                             2-1562 5 CONHCO -- 4-NH.sub.2 -Ph                                             2-1563 5 CONHCO -- 2-(HO.sub.3 S)Ph                                           2-1564 5 CONHCO -- 4-(HO.sub.3 S)Ph                                           2-1565 5 CONHCO -- 2-(NH.sub.2 O.sub.2 S)Ph                                   2-1566 5 CONHCO -- 4-9NH.sub.2 O.sub.2 S)Ph                                   2-1567 5 CONHCO -- 2-CN-Ph                                                    2-1568 5 CONHCO -- 4-CN-Ph                                                    2-1569 5 CONHCO -- 2-(HOCH.sub.2)Ph                                           2-1570 5 CONHCO -- 4-(HOCH.sub.2)Ph                                           2-1571 5 CONHCO -- Me                                                         2-1572 5 CONHCO -- Et                                                         2-1573 5 CONHCO -- Pr                                                         2-1574 5 CONHCO -- iPr                                                        2-1575 5 CONHCO -- Bu                                                         2-1576 5 CONHCO -- HOOCCH.sub.2 --                                            2-1577 5 CONHCO -- MeOOCCH.sub.2 --                                           2-1578 5 CONHCO -- MeCH(COOH)                                                 2-1579 5 CONHCO -- HOOC--(CH.sub.2).sub.2 --                                  2-1580 5 CONHCO -- MeCH(COOMe)                                                2-1581 5 CONHCO -- 1-HOOC-iBu                                                 2-1582 5 CONHCO -- 1-MeOOC-iBu                                                2-1583 5 CONHCO -- 1-HOOC-iPn                                                 2-1584 5 CONHCO -- 1-MeOOC-iPn                                                2-1585 5 CONHCO -- 1-HOOC-2-Me-Bu                                             2-1586 5 CONHCO -- 1-MeOOC-2-Me-Bu                                            2-1587 5 CONHCO -- CH.sub.2 CH.sub.2 SO.sub.3 H                               2-1588 5 CONHCO -- Z-1                                                        2-1589 5 CONHCO -- Z-2                                                        2-1590 5 CONHCO -- Z-3                                                        2-1591 5 CONHCO -- Z-4                                                        2-1592 5 CONHCO -- Z-5                                                        2-1593 5 CONHCO -- Z-6                                                        2-1594 5 CONHCO -- Z-7                                                        2-1595 5 CONHCO -- Z-8                                                        2-1596 5 CONHCO -- Z-9                                                        2-1597 5 CONHCO -- Z-10                                                       2-1598 5 CONHCO -- Z-11                                                       2-1599 5 CONHCO -- Z-12                                                       2-1600 5 CONHCO -- 3-Py                                                       2-1601 5 CONHCO -- 4-Py                                                       2-1602 5 CON(Ac)CO -- H                                                       2-1603 5 CON(Ac)CO -- Ph                                                      2-1604 5 CON(Ac)CO -- 2-Me-Ph                                                 2-1605 5 CON(Ac)CO -- 4-Me-Ph                                                 2-1606 5 CON(Ac)CO -- 2,4-diMe-Ph                                             2-1607 5 CON(Ac)CO -- 3,4-diMe-Ph                                             2-1608 5 CON(Ac)CO -- 2-(CF.sub.3)Ph                                          2-1609 5 CON(Ac)CO -- 4-(CF.sub.3)Ph                                          2-1610 5 CON(Ac)CO -- 2-MeOPh                                                 2-1611 5 CON(Ac)CO -- 4-MeOPh                                                 2-1612 5 CON(Ac)CO -- 2-EtOPh                                                 2-1613 5 CON(Ac)CO -- 4-EtOPh                                                 2-1614 5 CON(Ac)CO -- 2-HOPh                                                  2-1615 5 CON(Ac)CO -- 4-HOPh                                                  2-1616 5 CON(Ac)CO -- 2-(HOOC)Ph                                              2-1617 5 CON(Ac)CO -- 4-(HOOC)Ph                                              2-1618 5 CON(Ac)CO -- 2-(MeOOC)Ph                                             2-1619 5 CON(Ac)CO -- 4-(MeOOC)Ph                                             2-1620 5 CON(Ac)CO -- 2-(EtOOC)Ph                                             2-1621 5 CON(Ac)CO -- 4-(EtOOC)Ph                                             2-1622 5 CON(Ac)CO -- 2-(tBuOOC)Ph                                            2-1623 5 CON(Ac)CO -- 4-(tBuOOC)Ph                                            2-1624 5 CON(Ac)CO -- 2-Cl-Ph                                                 2-1625 5 CON(Ac)CO -- 4-Cl-Ph                                                 2-1626 5 CON(Ac)CO -- 2-Br-Ph                                                 2-1627 5 CON(Ac)CO -- 4-Br-Ph                                                 2-1628 5 CON(Ac)CO -- 2-I-Ph                                                  2-1629 5 CON(Ac)CO -- 4-I-Ph                                                  2-1630 5 CON(Ac)CO -- 2-NO.sub.2 -Ph                                          2-1631 5 CON(Ac)CO -- 4-NO.sub.2 -Ph                                          2-1632 5 CON(Ac)CO -- 2-NH.sub.2 -Ph                                          2-1633 5 CON(Ac)CO -- 4-NH.sub.2 -Ph                                          2-1634 5 CON(Ac)CO -- 2-(HO.sub.3 S)Ph                                        2-1635 5 CON(Ac)CO -- 4-(HO.sub.3 S)Ph                                        2-1636 5 CON(Ac)CO -- 2-(NH.sub.2 O.sub.2 S)Ph                                2-1637 5 CON(Ac)CO -- 4-(NH.sub.2 O.sub.2 S)Ph                                2-1638 5 CON(Ac)CO -- 2-CN-Ph                                                 2-1639 5 CON(Ac)CO -- 4-CN-Ph                                                 2-1640 5 CON(Ac)CO -- 2-(HOCH.sub.2)Ph                                        2-1641 5 CON(Ac)CO -- 4-(HOCH.sub.2)Ph                                        2-1642 5 CON(Ac)CO -- Me                                                      2-1643 5 CON(Ac)CO -- Et                                                      2-1644 5 CON(Ac)CO -- Pr                                                      2-1645 5 CON(Ac)CO -- iPr                                                     2-1646 5 CON(Ac)CO -- Bu                                                      2-1647 5 CON(Ac)CO -- HOOCCH.sub.2 --                                         2-1648 5 CON(Ac)CO -- MeOOCCH.sub.2 --                                        2-1649 5 CON(Ac)CO -- MeCH(COOH)                                              2-1650 5 CON(Ac)CO -- HOOC--(CH.sub.2).sub.2 --                               2-1651 5 CON(Ac)CO -- MeCH(COOMe)                                             2-1652 5 CON(Ac)CO -- 1-HOOC-iBu                                              2-1653 5 CON(Ac)CO -- 1-MeOOC-iBu                                             2-1654 5 CON(Ac)CO -- 1-HOOC-iPn                                              2-1655 5 CON(Ac)CO -- 1-MeOOC-iPn                                             2-1656 5 CON(Ac)CO -- 1-HOOC-2-Me-Bu                                          2-1657 5 CON(Ac)CO -- 1-MeOOC-2-Me-Bu                                         2-1658 5 CON(Ac)CO -- CH.sub.2 CH.sub.2 SO.sub.3 H                            2-1659 5 CON(Ac)CO -- Z-1                                                     2-1660 5 CON(Ac)CO -- Z-2                                                     2-1661 5 CON(Ac)CO -- Z-3                                                     2-1662 5 CON(Ac)CO -- Z-4                                                     2-1663 5 CON(Ac)CO -- Z-5                                                     2-1664 5 CON(Ac)CO -- Z-6                                                     2-1665 5 CON(Ac)CO -- Z-7                                                     2-1666 5 CON(Ac)CO -- Z-8                                                     2-1667 5 CON(Ac)CO -- Z-9                                                     2-1668 5 CON(Ac)CO -- Z-10                                                    2-1669 5 CON(Ac)CO -- Z-11                                                    2-1670 5 CON(Ac)CO -- Z-12                                                    2-1671 5 CON(Ac)CO -- 3-Py                                                    2-1672 5 CON(Ac)CO -- 4-Py                                                    2-1673 5 CONHCO NH H                                                          2-1674 5 CONHCO NH Ph                                                         2-1675 5 CONHCO NH 2-Me-Ph                                                    2-1676 5 CONHCO NH 4-Me-Ph                                                    2-1677 5 CONHCO NH 2,4-diMe-Ph                                                2-1678 5 CONHCO NH 3,4-diMe-Ph                                                2-1679 5 CONHCO NH 2-(CF.sub.3)Ph                                             2-1680 5 CONHCO NH 4-(CF.sub.3)Ph                                             2-1681 5 CONHCO NH 2-MeOPh                                                    2-1682 5 CONHCO NH 4-MeOPh                                                    2-1683 5 CONHCO NH 2-EtOPh                                                    2-1684 5 CONHCO NH 4-EtOPh                                                    2-1685 5 CONHCO NH 2-HOPh                                                     2-1686 5 CONHCO NH 4-HOPh                                                     2-1687 5 CONHCO NH 2-(HOOC)Ph                                                 2-1688 5 CONHCO NH 4-(HOOC)Ph                                                 2-1689 5 CONHCO NH 2-(MeOOC)Ph                                                2-1690 5 CONHCO NH 4-(MeOOC)Ph                                                2-1691 5 CONHCO NH 2-(EtOOC)Ph                                                2-1692 5 CONHCO NH 4-(EtOOC)Ph                                                2-1693 5 CONHCO NH 2-(tBuOOC)Ph                                               2-1694 5 CONHCO NH 4-(tBuOOC)Ph                                               2-1695 5 CONHCO NH 2-Cl-Ph                                                    2-1696 5 CONHCO NH 4-Cl-Ph                                                    2-1697 5 CONHCO NH 2-Br-Ph                                                    2-1698 5 CONHCO NH 4-Br-Ph                                                    2-1699 5 CONHCO NH 2-I-Ph                                                     2-1700 5 CONHCO NH 4-I-Ph                                                     2-1701 5 CONHCO NH 2-NO.sub.2 -Ph                                             2-1702 5 CONHCO NH 4-NO.sub.2 -Ph                                             2-1703 5 CONHCO NH 2-NH.sub.2 -Ph                                             2-1704 5 CONHCO NH 4-NH.sub.2 -Ph                                             2-1705 5 CONHCO NH 2-(HO.sub.3 S)Ph                                           2-1706 5 CONHCO NH 4-(HO.sub.3 S)Ph                                           2-1707 5 CONHCO NH 2-(NH.sub.2 O.sub.2 S)Ph                                   2-1708 5 CONHCO NH 4-(NH.sub.2 O.sub.2 S)Ph                                   2-1709 5 CONHCO NH 2-CN-Ph                                                    2-1710 5 CONHCO NH 4-CN-Ph                                                    2-1711 5 CONHCO NH 2-(HOCH.sub.2)Ph                                           2-1712 5 CONHCO NH 4-(HOCH.sub.2)Ph                                           2-1713 5 CONHCO NH Me                                                         2-1714 5 CONHCO NH Et                                                         2-1715 5 CONHCO NH Pr                                                         2-1716 5 CONHCO NH iPr                                                        2-1717 5 CONHCO NH Bu                                                         2-1718 5 CONHCO NH HOOCCH.sub.2 --                                            2-1719 5 CONHCO NH MeOOCCH.sub.2 --                                           2-1720 5 CONHCO NH MeCH(COOH)                                                 2-1721 5 CONHCO NH HOOC--(CH.sub.2).sub.2 --                                  2-1722 5 CONHCO NH MeCH(COOMe)                                                2-1723 5 CONHCO NH 1-HOOC-iBu                                                 2-1724 5 CONHCO NH 1-MeOOC-iBu                                                2-1725 5 CONHCO NH 1-HOOC-iPn                                                 2-1726 5 CONHCO NH 1-MeOOC-iPn                                                2-1727 5 CONHCO NH 1-HOOC-2-Me-Bu                                             2-1728 5 CONHCO NH 1-MeOOC-2-Me-Bu                                            2-1729 5 CONHCO NH CH.sub.2 CH.sub.2 SO.sub.3 H                               2-1730 5 CONHCO NH HO                                                         2-1731 5 CONHCO NH MeO                                                        2-1732 5 CONHCO NH EtO                                                        2-1733 5 CONHCO NH PrO                                                        2-1734 5 CONHCO NH iPrO                                                       2-1735 5 CONHCO NH BuO                                                        2-1736 5 CONHCO NH iBuO                                                       2-1737 5 CONHCO NH sBuO                                                       2-1738 5 CONHCO NH tBuO                                                       2-1739 5 CONHCO NH HxO                                                        2-1740 5 CONHCO NH PhO                                                        2-1741 5 CONHCO NH BnO                                                        2-1742 5 CONHCO NH Z-1                                                        2-1743 5 CONHCO NH Z-2                                                        2-1744 5 CONHCO NH Z-3                                                        2-1745 5 CONHCO NH Z-4                                                        2-1746 5 CONHCO NH Z-5                                                        2-1747 5 CONHCO NH Z-6                                                        2-1748 5 CONHCO NH Z-7                                                        2-1749 5 CONHCO NH Z-8                                                        2-1750 5 CONHCO NH Z-9                                                        2-1751 5 CONHCO NH Z-10                                                       2-1752 5 CONHCO NH Z-11                                                       2-1753 5 CONHCO NH Z-12                                                       2-1754 5 CONHCO NH 3-Py                                                       2-1755 5 CONHCO NH 4-Py                                                       2-1756 5 CONHSO.sub.2 -- H                                                    2-1757 5 CONHSO.sub.2 -- Ph                                                   2-1758 5 CONHSO.sub.2 -- 2-Me-Ph                                              2-1759 5 CONHSO.sub.2 -- 4-Me-Ph                                              2-1760 5 CONHSO.sub.2 -- 2,4-diMe-Ph                                          2-1761 5 CONHSO.sub.2 -- 3,4-diMe-Ph                                          2-1762 5 CONHSO.sub.2 -- 2-(CF.sub.3)Ph                                       2-1763 5 CONHSO.sub.2 -- 4-(CF.sub.3)Ph                                       2-1764 5 CONHSO.sub.2 -- 2-MeOPh                                              2-1765 5 CONHSO.sub.2 -- 4-MeOPh                                              2-1766 5 CONHSO.sub.2 -- 2-EtOPh                                              2-1767 5 CONHSO.sub.2 -- 4-EtOPh                                              2-1768 5 CONHSO.sub.2 -- 2-HOPh                                               2-1769 5 CONHSO.sub.2 -- 4-HOPh                                               2-1770 5 CONHSO.sub.2 -- 2-(HOOC)Ph                                           2-1771 5 CONHSO.sub.2 -- 4-(HOOC)Ph                                           2-1772 5 CONHSO.sub.2 -- 2-(MeOOC)Ph                                          2-1773 5 CONHSO.sub.2 -- 4-(MeOOC)Ph                                          2-1774 5 CONHSO.sub.2 -- 2-(EtOOC)Ph                                          2-1775 5 CONHSO.sub.2 -- 4-(EtOOC)Ph                                          2-1776 5 CONHSO.sub.2 -- 2-(tBuOOC)Ph                                         2-1777 5 CONHSO.sub.2 -- 4-(tBuOOC)Ph                                         2-1778 5 CONHSO.sub.2 -- 2-Cl-Ph                                              2-1779 5 CONHSO.sub.2 -- 4-Cl-Ph                                              2-1780 5 CONHSO.sub.2 -- 2-Br-Ph                                              2-1781 5 CONHSO.sub.2 -- 4-Br-Ph                                              2-1782 5 CONHSO.sub.2 -- 2-I-Ph                                               2-1783 5 CONHSO.sub.2 -- 4-I-Ph                                               2-1784 5 CONHSO.sub.2 -- 2-NO.sub.2 -Ph                                       2-1785 5 CONHSO.sub.2 -- 4-NO.sub.2 -Ph                                       2-1786 5 CONHSO.sub.2 -- 2-NH.sub.2 -Ph                                       2-1787 5 CONHSO.sub.2 -- 4-NH.sub.2 -Ph                                       2-1788 5 CONHSO.sub.2 -- 2-(HO.sub.3 S)Ph                                     2-1789 5 CONHSO.sub.2 -- 4-(HO.sub.3 S)Ph                                     2-1790 5 CONHSO.sub.2 -- 2-(NH.sub.2).sub.2 S)Ph                              2-1791 5 CONHSO.sub.2 -- 4-(NH.sub.2).sub.2 S)Ph                              2-1792 5 CONHSO.sub.2 -- 2-CN-Ph                                              2-1793 5 CONHSO.sub.2 -- 4-CN-Ph                                              2-1794 5 CONHSO.sub.2 -- 2-(HOCH.sub.2)Ph                                     2-1795 5 CONHSO.sub.2 -- 4-(HOCH.sub.2)Ph                                     2-1796 5 CONHSO.sub.2 -- Me                                                   2-1797 5 CONHSO.sub.2 -- Et                                                   2-1798 5 CONHSO.sub.2 -- Pr                                                   2-1799 5 CONHSO.sub.2 -- iPr                                                  2-1800 5 CONHSO.sub.2 -- Bu                                                   2-1801 5 CONHSO.sub.2 -- HOOCCH.sub.2 --                                      2-1802 5 CONHSO.sub.2 -- MeOOCCH.sub.2 --                                     2-1803 5 CONHSO.sub.2 -- MeCH(COOH)                                           2-1804 5 CONHSO.sub.2 -- HOOC--(CH.sub.2).sub.2 --                            2-1805 5 CONHSO.sub.2 -- MeCH(COOMe)                                          2-1806 5 CONHSO.sub.2 -- 1-HOOC-iBu                                           2-1807 5 CONHSO.sub.2 -- 1-MeOOC-iBu                                          2-1808 5 CONHSO.sub.2 -- 1-HOOC-iPn                                           2-1809 5 CONHSO.sub.2 -- 1-MeOOC-iPn                                          2-1810 5 CONHSO.sub.2 -- 1-HOOC-2-Me-Bu                                       2-1811 5 CONHSO.sub.2 -- 1-MeOOC-2-Me-Bu                                      2-1812 5 CONHSO.sub.2 -- CH.sub.2 CH.sub.2 SO.sub.3 H                         2-1813 5 CONHSO.sub.2 -- OH                                                   2-1814 5 CONHSO.sub.2 -- MeO                                                  2-1815 5 CONHSO.sub.2 -- EtO                                                  2-1816 5 CONHSO.sub.2 -- PrO                                                  2-1817 5 CONHSO.sub.2 -- iPrO                                                 2-1818 5 CONHSO.sub.2 -- BuO                                                  2-1819 5 CONHSO.sub.2 -- iBuO                                                 2-1820 5 CONHSO.sub.2 -- sBuO                                                 2-1821 5 CONHSO.sub.2 -- tBuO                                                 2-1822 5 CONHSO.sub.2 -- HxO                                                  2-1823 5 CONHSO.sub.2 -- PhO                                                  2-1824 5 CONHSO.sub.2 -- BnO                                                  2-1825 5 CONHSO.sub.2 -- Z-1                                                  2-1826 5 CONHSO.sub.2 -- Z-2                                                  2-1827 5 CONHSO.sub.2 -- Z-3                                                  2-1828 5 CONHSO.sub.2 -- Z-4                                                  2-1829 5 CONHSO.sub.2 -- Z-5                                                  2-1830 5 CONHSO.sub.2 -- Z-6                                                  2-1831 5 CONHSO.sub.2 -- Z-7                                                  2-1832 5 CONHSO.sub.2 -- Z-8                                                  2-1833 5 CONHSO.sub.2 -- Z-9                                                  2-1834 5 CONHSO.sub.2 -- Z-10                                                 2-1835 5 CONHSO.sub.2 -- Z-11                                                 2-1836 5 CONHSO.sub.2 -- Z-12                                                 2-1837 5 CONHSO.sub.2 -- 3-Py                                                 2-1838 5 CONHSO.sub.2 -- 4-Py                                                 2-1839 5 CONHSO.sub.2 NH H                                                    2-1840 5 CONHSO.sub.2 NH Ph                                                   2-1841 5 CONHSO.sub.2 NH 2-Me-Ph                                              2-1842 5 CONHSO.sub.2 NH 4-Me-Ph                                              2-1843 5 CONHSO.sub.2 NH 2,4-diMe-Ph                                          2-1844 5 CONHSO.sub.2 NH 3,4-diMe-Ph                                          2-1845 5 CONHSO.sub.2 NH 2-(CF.sub.3)Ph                                       2-1846 5 CONHSO.sub.2 NH 4-(CF.sub.3)Ph                                       2-1847 5 CONHSO.sub.2 NH 2-MeOPh                                              2-1848 5 CONHSO.sub.2 NH 4-MeOPh                                              2-1849 5 CONHSO.sub.2 NH 2-EtOPh                                              2-1850 5 CONHSO.sub.2 NH 4-EtOPh                                              2-1851 5 CONHSO.sub.2 NH 2-HOPh                                               2-1852 5 CONHSO.sub.2 NH 4-HOPh                                               2-1853 5 CONHSO.sub.2 NH 2-(HOOC)Ph                                           2-1854 5 CONHSO.sub.2 NH 4-(HOOC)Ph                                           2-1855 5 CONHSO.sub.2 NH 2-(MeOOC)Ph                                          2-1856 5 CONHSO.sub.2 NH 4-(MeOOC)Ph                                          2-1857 5 CONHSO.sub.2 NH 2-(EtOOC)Ph                                          2-1858 5 CONHSO.sub.2 NH 4-(EtOOC)Ph                                          2-1859 5 CONHSO.sub.2 NH 2-(tBuOOC)Ph                                         2-1860 5 CONHSO.sub.2 NH 4-(tBuOOC)Ph                                         2-1861 5 CONHSO.sub.2 NH 2-Cl-Ph                                              2-1862 5 CONHSO.sub.2 NH 4-Cl-Ph                                              2-1863 5 CONHSO.sub.2 NH 2-Br-Ph                                              2-1864 5 CONHSO.sub.2 NH 4-Br-Ph                                              2-1865 5 CONHSO.sub.2 NH 2-I-Ph                                               2-1866 5 CONHSO.sub.2 NH 4-I-Ph                                               2-1867 5 CONHSO.sub.2 NH 2-NO.sub.2 -Ph                                       2-1868 5 CONHSO.sub.2 NH 4-NO.sub.2 -Ph                                       2-1869 5 CONHSO.sub.2 NH 2-NH.sub.2 -Ph                                       2-1870 5 CONHSO.sub.2 NH 4-NH.sub.2 -Ph                                       2-1871 5 CONHSO.sub.2 NH 2-(HO.sub.3 S)Ph                                     2-1872 5 CONHSO.sub.2 NH 4-(HO.sub.3 S)Ph                                     2-1873 5 CONHSO.sub.2 NH 2-(NH.sub.2 O.sub.2 S)Ph                             2-1874 5 CONHSO.sub.2 NH 4-(NH.sub.2 O.sub.2 S)Ph                             2-1875 5 CONHSO.sub.2 NH 2-CN-Ph                                              2-1876 5 CONHSO.sub.2 NH 4-CN-Ph                                              2-1877 5 CONHSO.sub.2 NH 2-(HOCH.sub.2)Ph                                     2-1878 5 CONHSO.sub.2 NH 4-(HOCH.sub.2)Ph                                     2-1879 5 CONHSO.sub.2 NH Me                                                   2-1880 5 CONHSO.sub.2 NH Et                                                   2-1881 5 CONHSO.sub.2 NH Pr                                                   2-1882 5 CONHSO.sub.2 NH iPr                                                  2-1883 5 CONHSO.sub.2 NH Bu                                                   2-1884 5 CONHSO.sub.2 NH HOOCCH.sub.2 --                                      2-1885 5 CONHSO.sub.2 NH MeOOCCH.sub.2 --                                     2-1886 5 CONHSO.sub.2 NH MeCH(COOH)                                           2-1887 5 CONHSO.sub.2 NH HOOC--(CH.sub.2).sub.2 --                            2-1888 5 CONHSO.sub.2 NH MeCH(COOMe)                                          2-1889 5 CONHSO.sub.2 NH 1-HOOC-iBu                                           2-1890 5 CONHSO.sub.2 NH 1-MeOOC-iBu                                          2-1891 5 CONHSO.sub.2 NH 1-HOOC-iPn                                           2-1892 5 CONHSO.sub.2 NH 1-MeOOC-iPn                                          2-1893 5 CONHSO.sub.2 NH 1-HOOC-2-Me-Bu                                       2-1894 5 CONHSO.sub.2 NH 1-MeOOC-2-Me-Bu                                      2-1895 5 CONHSO.sub.2 NH CH.sub.2 CH.sub.2 SO.sub.3 H                         2-1896 5 CONHSO.sub.2 NH OH                                                   2-1897 5 CONHSO.sub.2 NH MeO                                                  2-1898 5 CONHSO.sub.2 NH EtO                                                  2-1899 5 CONHSO.sub.2 NH PrO                                                  2-1900 5 CONHSO.sub.2 NH iPrO                                                 2-1901 5 CONHSO.sub.2 NH BuO                                                  2-1902 5 CONHSO.sub.2 NH iBuO                                                 2-1903 5 CONHSO.sub.2 NH sBuO                                                 2-1904 5 CONHSO.sub.2 NH tBuO                                                 2-1905 5 CONHSO.sub.2 NH HxO                                                  2-1906 5 CONHSO.sub.2 NH PhO                                                  2-1907 5 CONHSO.sub.2 NH BnO                                                  2-1908 5 CONHSO.sub.2 NH Z-1                                                  2-1909 5 CONHSO.sub.2 NH Z-2                                                  2-1910 5 CONHSO.sub.2 NH Z-3                                                  2-1911 5 CONHSO.sub.2 NH Z-4                                                  2-1912 5 CONHSO.sub.2 NH Z-5                                                  2-1913 5 CONHSO.sub.2 NH Z-6                                                  2-1914 5 CONHSO.sub.2 NH Z-7                                                  2-1915 5 CONHSO.sub.2 NH Z-8                                                  2-1916 5 CONHSO.sub.2 NH Z-9                                                  2-1917 5 CONHSO.sub.2 NH Z-10                                                 2-1918 5 CONHSO.sub.2 NH Z-11                                                 2-1919 5 CONHSO.sub.2 NH Z-12                                                 2-1920 5 CONHSO.sub.2 NH 3-Py                                                 2-1921 5 CONHSO.sub.2 NH 4-Py                                                 2-1922 5 NHCO -- H                                                            2-1923 5 NHCO -- Ph                                                           2-1924 5 NHCO -- 2-Me-Ph                                                      2-1925 5 NHCO -- 4-Me-Ph                                                      2-1926 5 NHCO -- 2,4-diMe-Ph                                                  2-1927 5 NHCO -- 3,4-diMe-Ph                                                  2-1928 5 NHCO -- 2-(CF.sub.3)Ph                                               2-1929 5 NHCO -- 4-(CF.sub.3)Ph                                               2-1930 5 NHCO -- 2-MeOPh                                                      2-1931 5 NHCO -- 4-MeOPh                                                      2-1932 5 NHCO -- 2-EtOPh                                                      2-1933 5 NHCO -- 4-EtOPh                                                      2-1934 5 NHCO -- 2-HOPh                                                       2-1935 5 NHCO -- 4-HOPh                                                       2-1936 5 NHCO -- 2-(HOOC)Ph                                                   2-1937 5 NHCO -- 4-(HOOC)Ph                                                   2-1938 5 NHCO -- 2-(MeOOC)Ph                                                  2-1939 5 NHCO -- 4-(MeOOC)Ph                                                  2-1940 5 NHCO -- 2-(EtOOC)Ph                                                  2-1941 5 NHCO -- 4-(EtOOC)Ph                                                  2-1942 5 NHCO -- 2-(tBuOOC)Ph                                                 2-1943 5 NHCO -- 4-(tBuOOC)Ph                                                 2-1944 5 NHCO -- 2-Cl-Ph                                                      2-1945 5 NHCO -- 4-Cl-Ph                                                      2-1946 5 NHCO -- 2-Br-Ph                                                      2-1947 5 NHCO -- 4-Br-Ph                                                      2-1948 5 NHCO -- 2-I-Ph                                                       2-1949 5 NHCO -- 4-I-Ph                                                       2-1950 5 NHCO -- 2-NO.sub.2 -Ph                                               2-1951 5 NHCO -- 4-NO.sub.2 -Ph                                               2-1952 5 NHCO -- 2-NH.sub.2 -Ph                                               2-1953 5 NHCO -- 4-NH.sub.2 -Ph                                               2-1954 5 NHCO -- 2-(HO.sub.3 S)Ph                                             2-1955 5 NHCO -- 4-(HO.sub.3 S)Ph                                             2-1956 5 NHCO -- 2-(NH.sub.2 O.sub.2 S)Ph                                     2-1957 5 NHCO -- 4-(NH.sub.2 O.sub.2 S)Ph                                     2-1958 5 NHCO -- 2-CN-Ph                                                      2-1959 5 NHCO -- 4-CN-Ph                                                      2-1960 5 NHCO -- 2-(HOCH.sub.2)Ph                                             2-1961 5 NHCO -- 4-(HOCH.sub.2)Ph                                             2-1962 5 NHCO -- Me                                                           2-1963 5 NHCO -- Et                                                           2-1964 5 NHCO -- Pr                                                           2-1965 5 NHCO -- iPr                                                          2-1966 5 NHCO -- Bu                                                           2-1967 5 NHCO -- HOOCCH.sub.2 --                                              2-1968 5 NHCO -- MeOOCCH.sub.2 --                                             2-1969 5 NHCO -- MeCH(COOH)                                                   2-1970 5 NHCO -- HOOC--(CH.sub.2).sub.2 --                                    2-1971 5 NHCO -- MeCH(COOMe)                                                  2-1972 5 NHCO -- 1-HOOC-iBu                                                   2-1973 5 NHCO -- 1-HOOC-iPn                                                   2-1974 5 NHCO -- 1-HOOC-2-Me-Bu                                               2-1975 5 NHCO -- CH.sub.2 CH.sub.2 SO.sub.3 H                                 2-1976 5 NHCO -- MeO                                                          2-1977 5 NHCO -- EtO                                                          2-1978 5 NHCO -- PrO                                                          2-1979 5 NHCO -- Z-1                                                          2-1980 5 NHCO -- Z-2                                                          2-1981 5 NHCO -- Z-3                                                          2-1982 5 NHCO -- Z-4                                                          2-1983 5 NHCO -- Z-5                                                          2-1984 5 NHCO -- Z-6                                                          2-1985 5 NHCO -- Z-7                                                          2-1986 5 NHCO -- Z-8                                                          2-1987 5 NHCO -- Z-9                                                          2-1988 5 NHCO -- Z-10                                                         2-1989 5 NHCO -- Z-11                                                         2-1990 5 NHCO -- Z-12                                                         2-1991 5 NHCO -- 3-Py                                                         2-1992 5 NHCO -- 4-Py                                                         2-1993 5 NHCO NH H                                                            2-1994 5 NHCO NH Ph                                                           2-1995 5 NHCO NH 2-Me-Ph                                                      2-1996 5 NHCO NH 4-Me-Ph                                                      2-1997 5 NHCO NH 2,4-diMe-Ph                                                  2-1998 5 NHCO NH 3,4-diMe-Ph                                                  2-1999 5 NHCO NH 2-(CF.sub.3)Ph                                               2-2000 5 NHCO NH 4-(CF.sub.3)Ph                                               2-2001 5 NHCO NH 2-Me-Ph                                                      2-2002 5 NHCO NH 4-Me-Ph                                                      2-2003 5 NHCO NH 2-EtOPh                                                      2-2004 5 NHCO NH 4-EtOPh                                                      2-2005 5 NHCO NH 2-HOPh                                                       2-2006 5 NHCO NH 4-HOPh                                                       2-2007 5 NHCO NH 2-(HOOC)Ph                                                   2-2008 5 NHCO NH 4-(HOOC)Ph                                                   2-2009 5 NHCO NH 2-(MeOOC)Ph                                                  2-2010 5 NHCO NH 4-(MeOOC)Ph                                                  2-2011 5 NHCO NH 2-(EtOOC)Ph                                                  2-2012 5 NHCO NH 4-(EtOOC)Ph                                                  2-2013 5 NHCO NH 2-(tBuOOC)Ph                                                 2-2014 5 NHCO NH 4-(tBuOOC)Ph                                                 2-2015 5 NHCO NH 2-Cl-Ph                                                      2-2016 5 NHCO NH 4-Cl-Ph                                                      2-2017 5 NHCO NH 2-Br-Ph                                                      2-2018 5 NHCO NH 4-Br-Ph                                                      2-2019 5 NHCO NH 2-I-Ph                                                       2-2020 5 NHCO NH 4-I-Ph                                                       2-2021 5 NHCO NH 2-NO.sub.2 -Ph                                               2-2022 5 NHCO NH 4-NO.sub.2 -Ph                                               2-2023 5 NHCO NH 2-NH.sub.2 -Ph                                               2-2024 5 NHCO NH 4-NH.sub.2 -Ph                                               2-2025 5 NHCO NH 2-(HO.sub.3 S)Ph                                             2-2026 5 NHCO NH 4-(HO.sub.3 S)Ph                                             2-2027 5 NHCO NH 2-(NH.sub.2 O.sub.2 S)Ph                                     2-2028 5 NHCO NH 4-(NH.sub.2 O.sub.2 S)Ph                                     2-2029 5 NHCO NH 2-CN-Ph                                                      2-2030 5 NHCO NH 4-CN-Ph                                                      2-2031 5 NHCO NH 2-(HOCH.sub.2)Ph                                             2-2032 5 NHCO NH 4-(HOCH.sub.2)Ph                                             2-2033 5 NHCO NH Me                                                           2-2034 5 NHCO NH Et                                                           2-2035 5 NHCO NH Pr                                                           2-2036 5 NHCO NH iPr                                                          2-2037 5 NHCO NH Bu                                                           2-2038 5 NHCO NH HOOCCH.sub.2 --                                              2-2039 5 NHCO NH MeOOCCH.sub.2 --                                             2-2040 5 NHCO NH MeCH(COOH)                                                   2-2041 5 NHCO NH HOOC--(CH.sub.2).sub.2 --                                    2-2042 5 NHCO NH MeCH(COOMe)                                                  2-2043 5 NHCO NH 1-HOOC-iBu                                                   2-2044 5 NHCO NH 1-MeOOC-iBu                                                  2-2045 5 NHCO NH 1-HOOC-iPn                                                   2-2046 5 NHCO NH 1-MeOOC-iPn                                                  2-2047 5 NHCO NH 1-HOOC-2-Me-Bu                                               2-2048 5 NHCO NH 1-MeOOC-2-Me-Bu                                              2-2049 5 NHCO NH CH.sub.2 CH.sub.2 SO.sub.3 H                                 2-2050 5 NHCO NH OH                                                           2-2051 5 NHCO NH MeO                                                          2-2052 5 NHCO NH EtO                                                          2-2053 5 NHCO NH PrO                                                          2-2054 5 NHCO NH iPrO                                                         2-2055 5 NHCO NH BuO                                                          2-2056 5 NHCO NH iBuO                                                         2-2057 5 NHCO NH sBuO                                                         2-2058 5 NHCO NH tBuO                                                         2-2059 5 NHCO NH HxO                                                          2-2060 5 NHCO NH PhO                                                          2-2061 5 NHCO NH BnO                                                          2-2062 5 NHCO NH Z-1                                                          2-2063 5 NHCO NH Z-2                                                          2-2064 5 NHCO NH Z-3                                                          2-2065 5 NHCO NH Z-4                                                          2-2066 5 NHCO NH Z-5                                                          2-2067 5 NHCO NH Z-6                                                          2-2068 5 NHCO NH Z-7                                                          2-2069 5 NHCO NH Z-8                                                          2-2070 5 NHCO NH Z-9                                                          2-2071 5 NHCO NH Z-10                                                         2-2072 5 NHCO NH Z-11                                                         2-2073 5 NHCO NH Z-12                                                         2-2074 5 NHCO NH 3-Py                                                         2-2075 5 NHCO NH 4-Py                                                         2-2076 5 NHCO NMe Ph                                                          2-2077 5 NHCO NMe 2-Me-Ph                                                     2-2078 5 NHCO NMe 4-Me-Ph                                                     2-2079 5 NHCO NMe 2,4-diMe-Ph                                                 2-2080 5 NHCO NMe 3,4-diMe-Ph                                                 2-2081 5 NHCO NMe 2-(CF.sub.3)Ph                                              2-2082 5 NHCO NMe 4-(CF.sub.3)Ph                                              2-2083 5 NHCO NMe 2-MeOPh                                                     2-2084 5 NHCO NMe 4-MeOPh                                                     2-2085 5 NHCO NMe 2-EtOPh                                                     2-2086 5 NHCO NMe 4-EtOPh                                                     2-2087 5 NHCO NMe 2-HOPh                                                      2-2088 5 NHCO NMe 4-HOPh                                                      2-2089 5 NHCO NMe 2-(HOOC)Ph                                                  2-2090 5 NHCO NMe 4-(HOOC)Ph                                                  2-2091 5 NHCO NMe 2-(MeOOC)Ph                                                 2-2092 5 NHCO NMe 4-(MeOOC)Ph                                                 2-2093 5 NHCO NMe 2-(EtOOC)Ph                                                 2-2094 5 NHCO NMe 4-(EtOOC)Ph                                                 2-2095 5 NHCO NMe 2-(tBuOOC)Ph                                                2-2096 5 NHCO NMe 4-(tBuOOC)Ph                                                2-2097 5 NHCO NMe 2-Cl-Ph                                                     2-2098 5 NHCO NMe 4-Cl-Ph                                                     2-2099 5 NHCO NMe 2-Br-Ph                                                     2-2100 5 NHCO NMe 4-Br-Ph                                                     2-2101 5 NHCO NMe 2-I-Ph                                                      2-2102 5 NHCO NMe 4-I-Ph                                                      2-2103 5 NHCO NMe 2-NO.sub.2 -Ph                                              2-2104 5 NHCO NMe 4-NO.sub.2 -Ph                                              2-2105 5 NHCO NMe 2-NH.sub.2 -Ph                                              2-2106 5 NHCO NMe 4-NH.sub.2 -Ph                                              2-2107 5 NHCO NMe 2-(HO.sub.3 S)Ph                                            2-2108 5 NHCO NMe 4-(HO.sub.3 S)Ph                                            2-2109 5 NHCO NMe 2-(NH.sub.2 O.sub.2 S)Ph                                    2-2110 5 NHCO NMe 4-(NH.sub.2 O.sub.2 S)Ph                                    2-2111 5 NHCO NMe 2-CN-Ph                                                     2-2112 5 NHCO NMe 4-CN-Ph                                                     2-2113 5 NHCO NMe 2-(HOCH.sub.2)Ph                                            2-2114 5 NHCO NMe 4-(HOCH.sub.2)Ph                                            2-2115 5 NHCO NMe Me                                                          2-2116 5 NHCO NMe Et                                                          2-2117 5 NHCO NMe Pr                                                          2-2118 5 NHCO NMe iPr                                                         2-2119 5 NHCO NMe Bu                                                          2-2120 5 NHCO NMe HOOCCH.sub.2 --                                             2-2121 5 NHCO NMe MeOOCCH.sub.2 --                                            2-2122 5 NHCO NMe MeCH(COOH)                                                  2-2123 5 NHCO NMe HOOC--(CH.sub.2).sub.2 --                                   2-2124 5 NHCO NMe MeCH(COOMe)                                                 2-2125 5 NHCO NMe 1-HOOC-iBu                                                  2-2126 5 NHCO NMe 1-MeOOC-iBu                                                 2-2127 5 NHCO NMe 1-HOOC-iPn                                                  2-2128 5 NHCO NMe 1-MeOOC-iPn                                                 2-2129 5 NHCO NMe 1-HOOC-2-Me-Bu                                              2-2130 5 NHCO NMe 1-MeOOC-2-Me-Bu                                             2-2131 5 NHCO NMe CH.sub.2 CH.sub.2 SO.sub.3 H                                2-2132 5 NHCO NMe OH                                                          2-2133 5 NHCO NMe MeO                                                         2-2134 5 NHCO NMe EtO                                                         2-2135 5 NHCO NMe PrO                                                         2-2136 5 NHCO NMe iPrO                                                        2-2137 5 NHCO NMe BuO                                                         2-2138 5 NHCO NMe iBuO                                                        2-2139 5 NHCO NMe sBuO                                                        2-2140 5 NHCO NMe tBuO                                                        2-2141 5 NHCO NMe HxO                                                         2-2142 5 NHCO NMe PhO                                                         2-2143 5 NHCO NMe BnO                                                         2-2144 5 NHCO NMe Z-1                                                         2-2145 5 NHCO NMe Z-2                                                         2-2146 5 NHCO NMe Z-3                                                         2-2147 5 NHCO NMe Z-4                                                         2-2148 5 NHCO NMe Z-5                                                         2-2149 5 NHCO NMe Z-6                                                         2-2150 5 NHCO NMe Z-7                                                         2-2151 5 NHCO NMe Z-8                                                         2-2152 5 NHCO NMe Z-9                                                         2-2153 5 NHCO NMe Z-10                                                        2-2154 5 NHCO NMe Z-11                                                        2-2155 5 NHCO NMe Z-12                                                        2-2156 5 NHCO NMe 3-Py                                                        2-2157 5 NHCO NMe 4-Py                                                        2-2158 5 NHCO NHNH H                                                          2-2159 5 NHCO NHNH Me                                                         2-2160 5 NHCO NHNH Et                                                         2-2161 5 NHCO NHNME Me                                                        2-2162 5 NHCO NHNME Et                                                        2-2163 5 NHCO NHNME Pr                                                        2-2164 5 NHCONHNHCO NH H                                                      2-2165 5 NHCONHNHCO NH Ph                                                     2-2166 5 NHCONHNHCO NH 2-Me-Ph                                                2-2167 5 NHCONHNHCO NH 4-Me-Ph                                                2-2168 5 NHCONHNHCO NH 2,4-diMe-Ph                                            2-2169 5 NHCONHNHCO NH 3,4-diMe-Ph                                            2-2170 5 NHCONHNHCO NH 2-(CF.sub.3)Ph                                         2-2171 5 NHCONHNHCO NH 4-(CF.sub.3)Ph                                         2-2172 5 NHCONHNHCO NH 2-MeOPh                                                2-2173 5 NHCONHNHCO NH 4-MeOPh                                                2-2174 5 NHCONHNHCO NH 2-EtOPh                                                2-2175 5 NHCONHNHCO NH 4-EtOPh                                                2-2176 5 NHCONHNHCO NH 2-HOPh                                                 2-2177 5 NHCONHNHCO NH 4-HOPh                                                 2-2178 5 NHCONHNHCO NH 2-(HOOC)Ph                                             2-2179 5 NHCONHNHCO NH 4-(HOOC)Ph                                             2-2180 5 NHCONHNHCO NH 2-(MeOOC)Ph                                            2-2181 5 NHCONHNHCO NH 4-(MeOOC)Ph                                            2-2182 5 NHCONHNHCO NH 2-(EtOOC)Ph                                            2-2183 5 NHCONHNHCO NH 4-(EtOOC)Ph                                            2-2184 5 NHCONHNHCO NH 2-(tBuOOC)Ph                                           2-2185 5 NHCONHNHCO NH 4-(tBuOOC)Ph                                           2-2186 5 NHCONHNHCO NH 2-Cl-Ph                                                2-2187 5 NHCONHNHCO NH 4-Cl-Ph                                                2-2188 5 NHCONHNHCO NH 2-Br-Ph                                                2-2189 5 NHCONHNHCO NH 4-Br-Ph                                                2-2190 5 NHCONHNHCO NH 2-I-Ph                                                 2-2191 5 NHCONHNHCO NH 4-I-Ph                                                 2-2192 5 NHCONHNHCO NH 2-NO.sub.2 -Ph                                         2-2193 5 NHCONHNHCO NH 4-NO.sub.2 -Ph                                         2-2194 5 NHCONHNHCO NH 2-NH.sub.2 -Ph                                         2-2195 5 NHCONHNHCO NH 4-NH.sub.2 -Ph                                         2-2196 5 NHCONHNHCO NH 2-(HO.sub.3 S)Ph                                       2-2197 5 NHCONHNHCO NH 4-(HO.sub.3 S)Ph                                       2-2198 5 NHCONHNHCO NH 2-(NH.sub.2 O.sub.2 S)Ph                               2-2199 5 NHCONHNHCO NH 4-(NH.sub.2 O.sub.2 S)Ph                               2-2200 5 NHCONHNHCO NH 2-CN-Ph                                                2-2201 5 NHCONHNHCO NH 4-CN-Ph                                                2-2202 5 NHCONHNHCO NH 2-(HOCH.sub.2)Ph                                       2-2203 5 NHCONHNHCO NH 4-(HOCH.sub.2)Ph                                       2-2204 5 NHCONHNHCO NH Me                                                     2-2205 5 NHCONHNHCO NH Et                                                     2-2206 5 NHCONHNHCO NH Pr                                                     2-2207 5 NHCONHNHCO NH iPr                                                    2-2208 5 NHCONHNHCO NH Bu                                                     2-2209 5 NHCONHNHCO NH HOOCCH.sub.2 --                                        2-2210 5 NHCONHNHCO NH MeOOCCH.sub.2 --                                       2-2211 5 NHCONHNHCO NH MeCH(COOH)                                             2-2212 5 NHCONHNHCO NH HOOC--(CH.sub.2).sub.2 --                              2-2213 5 NHCONHNHCO NH MeCH(COOMe)                                            2-2214 5 NHCONHNHCO NH 1-HOOC-iBu                                             2-2215 5 NHCONHNHCO NH 1-MeOOC-iBu                                            2-2216 5 NHCONHNHCO NH 1-HOOC-iPn                                             2-2217 5 NHCONHNHCO NH 1-MeOOC-iPn                                            2-2218 5 NHCONHNHCO NH 1-HOOC-2-Me-Bu                                         2-2219 5 NHCONHNHCO NH 1-MeOOC-2-Me-Bu                                        2-2220 5 NHCONHNHCO NH CH.sub.2 CH.sub.2 SO.sub.3 H                           2-2221 5 NHCONHNHCO NH OH                                                     2-2222 5 NHCONHNHCO NH MeO                                                    2-2223 5 NHCONHNHCO NH EtO                                                    2-2224 5 NHCONHNHCO NH PrO                                                    2-2225 5 NHCONHNHCO NH iPrO                                                   2-2226 5 NHCONHNHCO NH BuO                                                    2-2227 5 NHCONHNHCO NH iBuO                                                   2-2228 5 NHCONHNHCO NH sBuO                                                   2-2229 5 NHCONHNHCO NH tBuO                                                   2-2230 5 NHCONHNHCO NH HxO                                                    2-2231 5 NHCONHNHCO NH PhO                                                    2-2232 5 NHCONHNHCO NH BnO                                                    2-2233 5 NHCONHNHCO NH Z-1                                                    2-2234 5 NHCONHNHCO NH Z-2                                                    2-2235 5 NHCONHNHCO NH Z-3                                                    2-2236 5 NHCONHNHCO NH Z-4                                                    2-2237 5 NHCONHNHCO NH Z-5                                                    2-2238 5 NHCONHNHCO NH Z-6                                                    2-2239 5 NHCONHNHCO NH Z-7                                                    2-2240 5 NHCONHNHCO NH Z-8                                                    2-2241 5 NHCONHNHCO NH Z-9                                                    2-2242 5 NHCONHNHCO NH Z-10                                                   2-2243 5 NHCONHNHCO NH Z-11                                                   2-2244 5 NHCONHNHCO NH Z-12                                                   2-2245 5 NHCONHNHCO NH 3-Py                                                   2-2246 5 NHCONHNHCO NH 4-Py                                                   2-2247 5 NHCONHCO -- H                                                        2-2248 5 NHCONHCO -- Ph                                                       2-2249 5 NHCONHCO -- 2-Me-Ph                                                  2-2250 5 NHCONHCO -- 4-Me-Ph                                                  2-2251 5 NHCONHCO -- 2,4-diMe-Ph                                              2-2252 5 NHCONHCO -- 3,4-diMe-Ph                                              2-2253 5 NHCONHCO -- 2-(CF.sub.3)Ph                                           2-2254 5 NHCONHCO -- 4-(CF.sub.3)Ph                                           2-2255 5 NHCONHCO -- 2-MeOPh                                                  2-2256 5 NHCONHCO -- 4-MeOPh                                                  2-2257 5 NHCONHCO -- 2-EtOPh                                                  2-2258 5 NHCONHCO -- 4-EtOPh                                                  2-2259 5 NHCONHCO -- 2-HOPh                                                   2-2260 5 NHCONHCO -- 4-HOPh                                                   2-2261 5 NHCONHCO -- 2-(HOOC)Ph                                               2-2262 5 NHCONHCO -- 4-(HOOC)Ph                                               2-2263 5 NHCONHCO -- 2-(MeOOC)Ph                                              2-2264 5 NHCONHCO -- 4-(MeOOC)Ph                                              2-2265 5 NHCONHCO -- 2-(EtOOC)Ph                                              2-2266 5 NHCONHCO -- 4-(EtOOC)Ph                                              2-2267 5 NHCONHCO -- 2-(tBuOOC)Ph                                             2-2268 5 NHCONHCO -- 4-(tBuOOC)Ph                                             2-2269 5 NHCONHCO -- 2-Cl-Ph                                                  2-2270 5 NHCONHCO -- 4-Cl-Ph                                                  2-2271 5 NHCONHCO -- 2-Br-Ph                                                  2-2272 5 NHCONHCO -- 4-Br-Ph                                                  2-2273 5 NHCONHCO -- 2-I-Ph                                                   2-2274 5 NHCONHCO -- 4-I-Ph                                                   2-2275 5 NHCONHCO -- 2-NO.sub.2 -Ph                                           2-2276 5 NHCONHCO -- 4-NO.sub.2 -Ph                                           2-2277 5 NHCONHCO -- 2-NH.sub.2 -Ph                                           2-2278 5 NHCONHCO -- 4-NH.sub.2 -Ph                                           2-2279 5 NHCONHCO -- 2-(HO.sub.3 S)Ph                                         2-2280 5 NHCONHCO -- 4-(HO.sub.3 S)Ph                                         2-2281 5 NHCONHCO -- 2-(NH.sub.2 O.sub.2 S)Ph                                 2-2282 5 NHCONHCO -- 4-(NH.sub.2 O.sub.2 S)Ph                                 2-2283 5 NHCONHCO -- 2-CN-Ph                                                  2-2284 5 NHCONHCO -- 4-CN-Ph                                                  2-2285 5 NHCONHCO -- 2-(HOCH.sub.2)Ph                                         2-2286 5 NHCONHCO -- 4-(HOCH.sub.2)Ph                                         2-2287 5 NHCONHCO -- Me                                                       2-2288 5 NHCONHCO -- Et                                                       2-2289 5 NHCONHCO -- Pr                                                       2-2290 5 NHCONHCO -- iPr                                                      2-2291 5 NHCONHCO -- Bu                                                       2-2292 5 NHCONHCO -- HOOCCH.sub.2 --                                          2-2293 5 NHCONHCO -- MeOOCCH.sub.2 --                                         2-2294 5 NHCONHCO -- MeCH(COOH)                                               2-2295 5 NHCONHCO -- HOOC--(CH.sub.2).sub.2 --                                2-2296 5 NHCONHCO -- MeCH(COOMe)                                              2-2297 5 NHCONHCO -- 1-HOOC-iBu                                               2-2298 5 NHCONHCO -- 1-MeOOC-iBu                                              2-2299 5 NHCONHCO -- 1-HOOC-iPn                                               2-2300 5 NHCONHCO -- 1-MeOOC-iPn                                              2-2301 5 NHCONHCO -- 1-HOOC-2-Me-Bu                                           2-2302 5 NHCONHCO -- 1-MeOOC-2-Me-Bu                                          2-2303 5 NHCONHCO -- CH.sub.2 CH.sub.2 SO.sub.3 H                             2-2304 5 NHCONHCO -- MeO                                                      2-2305 5 NHCONHCO -- EtO                                                      2-2306 5 NHCONHCO -- PrO                                                      2-2307 5 NHCONHCO -- iPrO                                                     2-2308 5 NHCONHCO -- BuO                                                      2-2309 5 NHCONHCO -- iBuO                                                     2-2310 5 NHCONHCO -- sBuO                                                     2-2311 5 NHCONHCO -- tBuO                                                     2-2312 5 NHCONHCO -- HxO                                                      2-2313 5 NHCONHCO -- PhO                                                      2-2314 5 NHCONHCO -- BnO                                                      2-2315 5 NHCONHCO -- Z-1                                                      2-2316 5 NHCONHCO -- Z-2                                                      2-2317 5 NHCONHCO -- Z-3                                                      2-2318 5 NHCONHCO -- Z-4                                                      2-2319 5 NHCONHCO -- Z-5                                                      2-2320 5 NHCONHCO -- Z-6                                                      2-2321 5 NHCONHCO -- Z-7                                                      2-2322 5 NHCONHCO -- Z-8                                                      2-2323 5 NHCONHCO -- Z-9                                                      2-2324 5 NHCONHCO -- Z-10                                                     2-2325 5 NHCONHCO -- Z-11                                                     2-2326 5 NHCONHCO -- Z-12                                                     2-2327 5 NHCONHCO -- 3-Py                                                     2-2328 5 NHCONHCO -- 4-Py                                                     2-2329 5 NHCONHSO.sub.2 -- H                                                  2-2330 5 NHCONHSO.sub.2 -- Ph                                                 2-2331 5 NHCONHSO.sub.2 -- 2-Me-Ph                                            2-2332 5 NHCONHSO.sub.2 -- 4-Me-Ph                                            2-2333 5 NHCONHSO.sub.2 -- 2,4-diMe-Ph                                        2-2334 5 NHCONHSO.sub.2 -- 3,4-diMe-Ph                                        2-2335 5 NHCONHSO.sub.2 -- 2-(CF.sub.3)Ph                                     2-2336 5 NHCONHSO.sub.2 -- 4-(CF.sub.3)Ph                                     2-2337 5 NHCONHSO.sub.2 -- 2-MeOPh                                            2-2338 5 NHCONHSO.sub.2 -- 4-MeOPh                                            2-2339 5 NHCONHSO.sub.2 -- 2-EtOPh                                            2-2340 5 NHCONHSO.sub.2 -- 4-EtOPh                                            2-2341 5 NHCONHSO.sub.2 -- 2-HOPh                                             2-2342 5 NHCONHSO.sub.2 -- 4-HOPh                                             2-2343 5 NHCONHSO.sub.2 -- 2-(HOOC)Ph                                         2-2344 5 NHCONHSO.sub.2 -- 4-(HOOC)Ph                                         2-2345 5 NHCONHSO.sub.2 -- 2-(MeOOC)Ph                                        2-2346 5 NHCONHSO.sub.2 -- 4-(MeOOC)Ph                                        2-2347 5 NHCONHSO.sub.2 -- 2-(EtOOC)Ph                                        2-2348 5 NHCONHSO.sub.2 -- 4-(EtOOC)Ph                                        2-2349 5 NHCONHSO.sub.2 -- 2-(tBuOOC)Ph                                       2-2350 5 NHCONHSO.sub.2 -- 4-(tBuOOC)Ph                                       2-2351 5 NHCONHSO.sub.2 -- 2-Cl-Ph                                            2-2352 5 NHCONHSO.sub.2 -- 4-Cl-Ph                                            2-2353 5 NHCONHSO.sub.2 -- 2-Br-Ph                                            2-2354 5 NHCONHSO.sub.2 -- 4-Br-Ph                                            2-2355 5 NHCONHSO.sub.2 -- 2-I-Ph                                             2-2356 5 NHCONHSO.sub.2 -- 4-I-Ph                                             2-2357 5 NHCONHSO.sub.2 -- 2-NO.sub.2 -Ph                                     2-2358 5 NHCONHSO.sub.2 -- 4-NO.sub.2 -Ph                                     2-2359 5 NHCONHSO.sub.2 -- 2-NH.sub.2 -Ph                                     2-2360 5 NHCONHSO.sub.2 -- 4-NH.sub.2 -Ph                                     2-2361 5 NHCONHSO.sub.2 -- 2-(HO.sub.3 S)Ph                                   2-2362 5 NHCONHSO.sub.2 -- 4-(HO.sub.3 S)Ph                                   2-2363 5 NHCONHSO.sub.2 -- 2-(NH.sub.2 O.sub.2 S)Ph                           2-2364 5 NHCONHSO.sub.2 -- 4-(NH.sub.2 O.sub.2 S)Ph                           2-2365 5 NHCONHSO.sub.2 -- 2-CN-Ph                                            2-2366 5 NHCONHSO.sub.2 -- 4-CN-Ph                                            2-2367 5 NHCONHSO.sub.2 -- 2-(HOCH.sub.2)Ph                                   2-2368 5 NHCONHSO.sub.2 -- 4-(HOCH.sub.2)Ph                                   2-2369 5 NHCONHSO.sub.2 -- Me                                                 2-2370 5 NHCONHSO.sub.2 -- Et                                                 2-2371 5 NHCONHSO.sub.2 -- Pr                                                 2-2372 5 NHCONHSO.sub.2 -- iPr                                                2-2373 5 NHCONHSO.sub.2 -- Bu                                                 2-2374 5 NHCONHSO.sub.2 -- HOOCCH.sub.2                                       2-2375 5 NHCONHSO.sub.2 -- MeOOCCH.sub.2                                      2-2376 5 NHCONHSO.sub.2 -- MeCH(COOH)                                         2-2377 5 NHCONHSO.sub.2 -- HOOC--(CH.sub.2).sub.2                             2-2378 5 NHCONHSO.sub.2 -- MeCH(COOMe)                                        2-2379 5 NHCONHSO.sub.2 -- 1-HOOC-iBu                                         2-2380 5 NHCONHSO.sub.2 -- 1-MeOOC-iPn                                        2-2381 5 NHCONHSO.sub.2 -- 1-HOOC-iPn                                         2-2382 5 NHCONHSO.sub.2 -- 1-MeOOC-iPn                                        2-2383 5 NHCONHSO.sub.2 -- 1-HOOC-2-Me-Bu                                     2-2384 5 NHCONHSO.sub.2 -- 1-MeOOC-2-Me-Bu                                    2-2385 5 NHCONHSO.sub.2 -- CH.sub.2 CH.sub.2 SO.sub.3 H                       2-2386 5 NHCONHSO.sub.2 -- OH                                                 2-2387 5 NHCONHSO.sub.2 -- MeO                                                2-2388 5 NHCONHSO.sub.2 -- EtO                                                2-2389 5 NHCONHSO.sub.2 -- PrO                                                2-2390 5 NHCONHSO.sub.2 -- iPrO                                               2-2391 5 NHCONHSO.sub.2 -- BuO                                                2-2392 5 NHCONHSO.sub.2 -- iBuO                                               2-2393 5 NHCONHSO.sub.2 -- sBuO                                               2-2394 5 NHCONHSO.sub.2 -- tBuO                                               2-2395 5 NHCONHSO.sub.2 -- HxO                                                2-2396 5 NHCONHSO.sub.2 -- PhO                                                2-2397 5 NHCONHSO.sub.2 -- BnO                                                2-2398 5 NHCONHSO.sub.2 -- Z-1                                                2-2399 5 NHCONHSO.sub.2 -- Z-2                                                2-2400 5 NHCONHSO.sub.2 -- Z-3                                                2-2401 5 NHCONHSO.sub.2 -- Z-4                                                2-2402 5 NHCONHSO.sub.2 -- Z-5                                                2-2403 5 NHCONHSO.sub.2 -- Z-6                                                2-2404 5 NHCONHSO.sub.2 -- Z-7                                                2-2405 5 NHCONHSO.sub.2 -- Z-8                                                2-2406 5 NHCONHSO.sub.2 -- Z-9                                                2-2407 5 NHCONHSO.sub.2 -- Z-10                                               2-2408 5 NHCONHSO.sub.2 -- Z-11                                               2-2409 5 NHCONHSO.sub.2 -- Z-12                                               2-2410 5 NHCONHSO.sub.2 -- 3-Py                                               2-2411 5 NHCONHSO.sub.2 -- 4-Py                                               2-2412 5 NHCONHSO.sub.2 NH H                                                  2-2413 5 NHCONHSO.sub.2 NH Me                                                 2-2414 5 NHCONHSO.sub.2 NH Et                                                 2-2415 5 NHCONHSO.sub.2 NH Pr                                                 2-2416 5 NHCONHSO.sub.2 NH iPr                                                2-2417 5 NHCONHSO.sub.2 NH Bu                                                 2-2418 5 NHCONHSO.sub.2 NMe Me                                                2-2419 5 NHCONHSO.sub.2 NMe Et                                                2-2420 5 NHCONHSO.sub.2 NMe Pr                                                2-2421 5 NHCONHSO.sub.2 NMe iPr                                               2-2422 5 NHCONHSO.sub.2 NMe Bu                                                2-2423 5 -- NH H                                                              2-2424 5 -- NH Me                                                             2-2425 5 -- NH Et                                                             2-2426 5 -- NH Pr                                                             2-2427 5 -- NH iPr                                                            2-2428 5 -- NH Bu                                                           2-2429                                                                              5     CO            Pyr                                                   2-2430 5 CO Pipri                                                             2-2431 5 CO Pipra                                                             2-2432 5 CO Mor                                                               2-2433 5 CO Thmor                                                             2-2434 5 CO NHPyr                                                             2-2435 5 CO NHPipri                                                           2-2436 5 CO NHPipra                                                           2-2437 5 CO NHMor                                                             2-2438 5 CO NHThmor                                                           2-2439 5 NHCO Pyr                                                             2-2440 5 NHCO Pipri                                                           2-2441 5 NHCO Pipra                                                           2-2442 5 NHCO Mor                                                             2-2443 5 NHCO Thmor                                                           2-2444 5 NHCO NHPyr                                                           2-2445 5 NHCO NHPipri                                                         2-2446 5 NHCO NHPipra                                                         2-2447 5 NHCO NHMor                                                           2-2448 5 NHCO NHThmor                                                         2-2449 5 CONHCO Pyr                                                           2-2450 5 CONHCO Pipri                                                         2-2451 5 CONHCO Pipra                                                         2-2452 5 CONHCO Mor                                                           2-2453 5 CONHCO Thmor                                                         2-2454 5 CONHCO NHPyr                                                         2-2455 5 CONHCO NHPipri                                                       2-2456 5 CONHCO NHPipra                                                       2-2457 5 CONHCO NHMor                                                         2-2458 5 CONHCO NHThmor                                                       2-2459 5 CONHSO.sub.2 Pyr                                                     2-2460 5 CONHSO.sub.2 Pipri                                                   2-2461 5 CONHSO.sub.2 Pipra                                                   2-2462 5 CONHSO.sub.2 Mor                                                     2-2463 5 CONHSO.sub.2 Thmor                                                   2-2464 5 CONHSO.sub.2 NHPyr                                                   2-2465 5 CONHSO.sub.2 NHPipri                                                 2-2466 5 CONHSO.sub.2 NHPipra                                                 2-2467 5 CONHSO.sub.2 NHMor                                                   2-2468 5 CONHSO.sub.2 NHThmor                                               2-2469                                                                              5     NHSO.sub.2    NH    Z-4                                             2-2470 5 NHSO.sub.2 -- Me                                                     2-2471 5 NHSO.sub.2 -- Et                                                     2-2472 5 NHSO.sub.2 -- Pr                                                     2-2473 5 NHSO.sub.2 -- CH.sub.2 --Cl                                          2-2474 5 NHSO.sub.2 -- Ph                                                     2-2475 5 NHSO.sub.2 -- 4-Me-Ph                                                2-2476 5 CO NMe Ph                                                            2-2477 5 CO NMe 2-Me-Ph                                                       2-2478 5 CO NMe 4-Me-Ph                                                       2-2479 5 CO NMe 2,4-diMe-Ph                                                   2-2480 5 CO NMe 3,4-diMe-Ph                                                   2-2481 5 CO NMe 2-(CF.sub.3)Ph                                                2-2482 5 CO NMe 4-(CF.sub.3)Ph                                                2-2483 5 CO NMe 2-MeOPh                                                       2-2484 5 CO NMe 4-MeOPh                                                       2-2485 5 CO NMe 2-EtOPh                                                       2-2486 5 CO NMe 4-EtOPh                                                       2-2487 5 CO NMe 2-HOPh                                                        2-2488 5 CO NMe 4-HOPh                                                        2-2489 5 CO NMe 2-(HOOC)Ph                                                    2-2490 5 CO NMe 4-(HOOC)Ph                                                    2-2491 5 CO NMe 2-(MeOOC)Ph                                                   2-2492 5 CO NMe 4-(MeOOC)Ph                                                   2-2493 5 CO NMe 2-(EtOOC)Ph                                                   2-2494 5 CO NMe 4-(EtOOC)Ph                                                   2-2495 5 CO NMe 2-(tBuOOC)Ph                                                  2-2496 5 CO NMe 4-(tBuOOC)Ph                                                  2-2497 5 CO NMe 2-Cl-Ph                                                       2-2498 5 CO NMe 4-Cl-Ph                                                       2-2499 5 CO NMe 2-Br-Ph                                                       2-2500 5 CO NMe 4-Br-Ph                                                       2-2501 5 CO NMe 2-I-Ph                                                        2-2502 5 CO NMe 4-I-Ph                                                        2-2503 5 CO NMe 2-NO.sub.2 -Ph                                                2-2504 5 CO NMe 4-NO.sub.2 -Ph                                                2-2505 5 CO NMe 2-NH.sub.2 -Ph                                                2-2506 5 CO NMe 4-NH.sub.2 -Ph                                                2-2507 5 CO NMe 2-(HO.sub.3 S)Ph                                              2-2508 5 CO NMe 4-(HO.sub.3 S)Ph                                              2-2509 5 CO NMe 2-(NH.sub.2 O.sub.2 S)Ph                                      2-2510 5 CO NMe 4-(NH.sub.2 O.sub.2 S)Ph                                      2-2511 5 CO NMe 2-CN-Ph                                                       2-2512 5 CO NMe 4-CN-Ph                                                       2-2513 5 CO NMe 2-(HOCH.sub.2)Ph                                              2-2514 5 CO NMe 4-(HOCH.sub.2)Ph                                              2-2515 5 CO NMe Me                                                            2-2516 5 CO NMe Et                                                            2-2517 5 CO NMe Pr                                                            2-2518 5 CO NMe iPr                                                           2-2519 5 CO NMe Bu                                                            2-2520 5 CO NMe HOOCCH.sub.2                                                  2-2521 5 CO NMe HOOC--(CH.sub.2).sub.2                                        2-2522 5 CO NMe MeCH(COOH)                                                    2-2523 5 CO NMe HOOC--(CH.sub.2).sub.3 --                                     2-2524 5 CO NMe MeCH(COOMe)                                                   2-2525 5 CO NMe 1-HOOC-iBu                                                    2-2526 5 CO NMe 1-MeOOC-iBu                                                   2-2527 5 CO NMe 1-HOOC-iPn                                                    2-2528 5 CO NMe 1-MeOOC-iPn                                                   2-2529 5 CO NMe 1-HOOC-2-Me-Bu                                                2-2530 5 CO NMe 1-MeOOC-2-Me-Bu                                               2-2531 5 CO NMe CH.sub.2 CH.sub.2 SO.sub.3 H                                  2-2532 5 CO NMe OH                                                            2-2533 5 CO NMe MeO                                                           2-2534 5 CO NMe EtO                                                           2-2535 5 CO NMe PrO                                                           2-2536 5 CO NMe iPrO                                                          2-2537 5 CO NMe BuO                                                           2-2538 5 CO NMe iBuO                                                          2-2539 5 CO NMe sBuO                                                          2-2540 5 CO NMe tBuO                                                          2-2541 5 CO NMe HxO                                                           2-2542 5 CO NMe PhO                                                           2-2543 5 CO NMe BnO                                                           2-2544 5 CO NMe Z-1                                                           2-2545 5 CO NMe Z-2                                                           2-2546 5 CO NMe Z-3                                                           2-2547 5 CO NMe Z-4                                                           2-2548 5 CO NMe Z-5                                                           2-2549 5 CO NMe Z-6                                                           2-2550 5 CO NMe Z-7                                                           2-2551 5 CO NMe Z-8                                                           2-2552 5 CO NMe Z-9                                                           2-2553 5 CO NMe Z-10                                                          2-2554 5 CO NMe Z-11                                                          2-2555 5 CO NMe Z-12                                                          2-2556 5 CO NMe 3-Py                                                          2-2557 5 CO NMe 4-Py                                                        2-2558                                                                              5     CO            Thiad                                                 2-2559 5 CO NHThiad                                                           2-2560 5 NHCO Thiad                                                           2-2561 5 NHCO NHThiad                                                         2-2562 5 CONHCO Thiad                                                         2-2563 5 CONHCO NHThiad                                                       2-2564 5 CONHSO.sub.2 Thiad                                                   2-2565 5 CONHSO.sub.2 NHThiad                                               2-2566                                                                              5     NHCS          NH    H                                               2-2567 5 NHCS NH Me                                                           2-2568 5 NHCS NH Et                                                           2-2569 5 NHCS NH Ph                                                           2-2570 5 NHCS NH HOOCCH.sub.2                                                 2-2571 5 NHCS NH MeOOCCH.sub.2                                                2-2572 5 NHCS NH MeCH(COOH)                                                   2-2573 5 NHCS NH HOOC--(CH.sub.2).sub.2                                       2-2574 5 NHCS NH MeCH(COOMe)                                                  2-2575 5 CO NH HOOC--(CH.sub.2).sub.3 --                                      2-2576 5 NHCO NH HOOC--(CH.sub.2).sub.3 --                                    2-2577 5 NHCO -- HOOC--(CH.sub.2).sub.3 --                                    2-2578 5 NHCS NH HOOC--(CH.sub.2).sub.3 --                                    2-2579 5 CO NH MeSO.sub.2 NHCOCH(Me)                                          2-2580 5 NHCO NH MeSO.sub.2 NHCOCH(Me)                                        2-2581 5 NHCO -- MeSO.sub.2 NHCOCH(Me)                                        2-2582 5 NHCS NH MeSO.sub.2 NHCOCH(Me)                                        2-2583 5 -- NH HOOCCH.sub.2                                                   2-2584 5 -- NH MeOOCCH.sub.2                                                  2-2585 5 -- NH MeCH(COOH)                                                     2-2586 5 -- NH HOOC--(CH.sub.2).sub.2                                         2-2587 5 -- NH MeCH(COOMe)                                                    2-2588 5 -- NH HOOC--(CH.sub.2).sub.3 --                                      2-2589 5 NHCOCO -- OH                                                         2-2590 5 NHCOCO -- MeO                                                        2-2591 5 NHCOCO -- EtO                                                        2-2592 5 NHCOCO -- PrO                                                        2-2593 5 NHCOCO -- iPrO                                                       2-2594 5 NHCOCO -- BuO                                                        2-2595 5 NHCOCO -- iBuO                                                       2-2596 5 NHCOCO -- sBuO                                                       2-2597 5 NHCOCO -- tBuO                                                       2-2598 5 NHCOCO -- HxO                                                        2-2599 5 NHCOCO -- PhO                                                        2-2600 5 NHCOCO -- BnO                                                      2-2601                                                                              0     --            1,3-diox-IInd                                         2-2602 1 -- 1,3-diox-IInd                                                     2-2603 2 -- 1,3-diox-IInd                                                     2-2604 3 -- 1,3-diox-IInd                                                     2-2605 4 -- 1,3-diox-IInd                                                     2-2606 5 -- 1,3-diox-IInd                                                     2-2607 6 -- 1,3-diox-IInd                                                     2-2608 7 -- 1,3-diox-IInd                                                     2-2609 8 -- 1,3-diox-IInd                                                     2-2610 9 -- 1,3-diox-IInd                                                     2-2611 10 -- 1,3-diox-IInd                                                    2-2612 11 -- 1,3-diox-IInd                                                    2-2613 12 -- 1,3-diox-IInd                                                  2-2614                                                                              4     NHCONHSO.sub.2 NHCO                                                                         NH    Z-4                                             2-2615 4 NHCONHSO.sub.2 NHCO NH Pn                                            2-2616 2 O -- H                                                               2-2617 4 O -- H                                                               2-2618 5 O -- H                                                               2-2619 5 O -- Ph                                                              2-2620 5 O -- 2-Py                                                            2-2621 5 O -- 3-Py                                                            2-2622 5 O -- 4-Py                                                            2-2623 5 O -- Z-1                                                             2-2624 5 O -- Z-2                                                             2-2625 5 O -- Z-3                                                             2-2626 5 O -- Z-4                                                             2-2627 5 O -- Z-5                                                             2-2628 5 O -- Z-6                                                             2-2629 5 O -- Z-7                                                             2-2630 5 O -- Z-8                                                             2-2631 5 O -- Z-9                                                             2-2632 5 O -- Z-10                                                            2-2633 5 O -- Z-11                                                            2-2634 5 O -- Z-12                                                            2-2635 4 NHCO -- 3-Py                                                         2-2636 5 NHCO -- 3-Py                                                         2-2637 4 CO NH HOCH.sub.2 CH(CH.sub.3)CH.sub.2                                2-2638 5 CO NH HOCH.sub.2 CH(CH.sub.3)CH.sub.2                                2-2639 4 NHCO NH HOCH.sub.2 CH(CH.sub.3)CH.sub.2                              2-2640 5 NHCO NH HOCH.sub.2 CH(CH.sub.3)CH.sub.2                              2-2641 4 CO NH MeSO.sub.2 NHCOCH.sub.2                                        2-2642 5 CO NH MeSO.sub.2 NHCOCH.sub.2                                        2-2643 4 NHCO NH MeSO.sub.2 NHCOCH.sub.2                                      2-2644 5 NHCO NH MeSO.sub.2 NHCOCH.sub.2                                      2-2645 4 CO NH H.sub.2 NSO.sub.2 NHCOCH.sub.2                                 2-2646 5 CO NH H.sub.2 NSO.sub.2 NHCOCH.sub.2                                 2-2647 4 NHCO NH H.sub.2 NSO.sub.2 NHCOCH.sub.2                               2-2648 5 CO NH H.sub.2 NSO.sub.2 NHCOCH.sub.2                                 2-2649 4 CO NH 1-(MeSO.sub.2 NHCO)-Et                                         2-2650 5 CO NH 1-(MeSO.sub.2 NHCO)-Et                                         2-2651 4 NHCO NH 1-(MeSO.sub.2 NHCO)-Et                                       2-2652 5 NHCO NH 1-(MeSO.sub.2 NHCO)-Et                                       2-2653 4 CO NH 1-(H.sub.2 NSO.sub.2 NHCO)-Et                                  2-2654 5 CO NH 1-(H.sub.2 NSO.sub.2 NHCO)-Et                                  2-2655 4 NHCO NH 1-(H.sub.2 NSO.sub.2 NHCO)-Et                                2-2656 5 NHCO NH 1-(H.sub.2 NSO.sub.2 NHCO)-Et                                2-2657 4 CO NH HOOC--(CH.sub.2).sub.4                                         2-2658 5 CO NH HOOC--(CH.sub.2).sub.4                                         2-2659 4 NHCO NH HOOC--(CH.sub.2).sub.4                                       2-2660 5 NHCO NH HOOC--(CH.sub.2).sub.4                                       2-2661 4 CO NH HO--(CH.sub.2).sub.2                                           2-2662 5 CO NH HO--(CH.sub.2).sub.2                                           2-2663 4 NHCO NH HO--(CH.sub.2).sub.2                                         2-2664 5 NHCO NH HO--(CH.sub.2).sub.2                                         2-2665 4 CO NH HO--CH.sub.2 --CH(CH.sub.3)                                    2-2666 5 CO NH HO--CH.sub.2 --CH(CH.sub.3)                                    2-2667 4 NHCO NH HO--CH.sub.2 --CH(CH.sub.3)                                  2-2668 5 NHCO NH HO--CH.sub.2 --CH(CH.sub.3)                                  2-2669 4 CO NMe HOOC--(CH.sub.2).sub.3                                        2-2670 4 NHCO NMe HOOC--(CH.sub.2).sub.3                                      2-2671 5 NHCO NMe HOOC--(CH.sub.2).sub.3                                      2-2672 4 CONMeSO.sub.2 -- Me                                                  2-2673 5 CONMeSO.sub.2 -- Me                                                2-2674                                                                              4     CO            1-Indn                                                2-2675 5 CO 1-Indn                                                            2-2676 4 NHCO 1-Indn                                                          2-2677 5 NHCO 1-Indn                                                          2-2678 4 CO 2-(HOOC)-1-Indn                                                   2-2679 5 CO 2-(HOOC)-1-Indn                                                   2-2680 4 NHCO 2-(HOOC)-1-Indn                                                 2-2681 5 NHCO 2-(HOOC)-1-Indn                                                 2-2682 4 -- 3,4-diMe-2,5-diox-1-Imdd                                          2-2683 5 -- 3,4-diMe-2,5-diox-1-Imdd                                        ______________________________________                                         ##STR7##

                  TABLE 3                                                         ______________________________________                                        Cpd.                                                                            No. k A B R.sup.1                                                           ______________________________________                                        3-1   4     CO             NH   H                                               3-2 4 CO NH Ph                                                                3-3 4 CO NH 2-Me--Ph                                                          3-4 4 CO NH 4-Me--Ph                                                          3-5 4 CO NH 2,4-diMe--Ph                                                      3-6 4 CO NH 3,4-diMe--Ph                                                      3-7 4 CO NH 2-(CF.sub.3)--Ph                                                  3-8 4 CO NH 4-(CF.sub.3)--Ph                                                  3-9 4 CO NH 2-MeOPh                                                           3-10 4 CO NH 4-MeOPh                                                          3-11 4 CO NH 2-EtOPh                                                          3-12 4 CO NH 4-EtOPh                                                          3-13 4 CO NH 2-HOPh                                                           3-14 4 CO NH 4-HOPh                                                           3-15 4 CO NH 2-(HOOC)--Ph                                                     3-16 4 CO NH 4-(HOOC)--Ph                                                     3-17 4 CO NH 2-(MeOOC)--Ph                                                    3-18 4 CO NH 4-(MeOOC)--Ph                                                    3-19 4 CO NH 2-(EtOOC)--Ph                                                    3-20 4 CO NH 4-(EtOOC)--Ph                                                    3-21 4 CO NH 2-(tBuOOC)--Ph                                                   3-22 4 CO NH 4-(tBuOOC)--Ph                                                   3-23 4 CO NH 2-Cl--Ph                                                         3-24 4 CO NH 4-Cl--Ph                                                         3-25 4 CO NH 2-Br--Ph                                                         3-26 4 CO NH 4-Br--Ph                                                         3-27 4 CO NH 2-I--Ph                                                          3-28 4 CO NH 4-I--Ph                                                          3-29 4 CO NH 2-NO.sub.2 --Ph                                                  3-30 4 CO NH 4-NO.sub.2 --Ph                                                  3-31 4 CO NH 2-NH.sub.2 --Ph                                                  3-32 4 CO NH 4-NH.sub.2 --Ph                                                  3-33 4 CO NH 2-(HO.sub.3 S)--Ph                                               3-34 4 CO NH 4-(HO.sub.3 S)--Ph                                               3-35 4 CO NH 2-(NH.sub.2 O.sub.2 S)--Ph                                       3-36 4 CO NH 4-(NH.sub.2 O.sub.2 S)--Ph                                       3-37 4 CO NH 2-CN--Ph                                                         3-38 4 CO NH 4-CN--Ph                                                         3-39 4 CO NH 2-(HOCH.sub.2)--Ph                                               3-40 4 CO NH 4-(HOCH.sub.2)--Ph                                               3-41 4 CO NH Me                                                               3-42 4 CO NH Et                                                               3-43 4 CO NH Pr                                                               3-44 4 CO NH iPr                                                              3-45 4 CO NH Bu                                                               3-46 4 CO NH HOOCCH.sub.2 --                                                  3-47 4 CO NH MeOOCCH.sub.2 --                                                 3-48 4 CO NH MeCH(COOH)--                                                     3-49 4 CO NH HOOC--(CH.sub.2).sub.2 --                                        3-50 4 CO NH MeCH(COOMe)-                                                     3-51 4 CO NH 1-HOOC-iBu                                                       3-52 4 CO NH 1-MeOOC-iBu                                                      3-53 4 CO NH 1-HOOC-iPn                                                       3-54 4 CO NH 1-MeOOC-iPn                                                      3-55 4 CO NH 1-HOOC-2-Me--Bu                                                  3-56 4 CO NH 1-MeOOC-2-Me--Bu                                                 3-57 4 CO NH CH.sub.2 CH.sub.2 SO.sub.3 H                                     3-58 4 CO NH OH                                                               3-59 4 CO NH MeO                                                              3-60 4 CO NH EtO                                                              3-61 4 CO NH Pro                                                              3-62 4 CO NH iPro                                                             3-63 4 CO NH BuO                                                              3-64 4 CO NH iBuO                                                             3-65 4 CO NH sBuO                                                             3-66 4 CO NH tBuO                                                             3-67 4 CO NH HxO                                                              3-68 4 CO NH PhO                                                              3-69 4 CO NH BnO                                                              3-70 4 CO NH Z-1                                                              3-71 4 CO NH Z-2                                                              3-72 4 CO NH Z-3                                                              3-73 4 CO NH Z-4                                                              3-74 4 CO NH Z-5                                                              3-75 4 CO NH Z-6                                                              3-76 4 CO NH Z-7                                                              3-77 4 CO NH Z-8                                                              3-78 4 CO NH Z-9                                                              3-79 4 CO NH Z-10                                                             3-80 4 CO NH Z-11                                                             3-81 4 CO NH Z-12                                                             3-82 4 CO NH 3-Py                                                             3-83 4 CO NH 4-Py                                                             3-84 4 CO N(Ac) H                                                             3-85 4 CO N(Ac) Ph                                                            3-86 4 CO N(Ac) 2-Me--Ph                                                      3-87 4 CO N(Ac) 4-Me--Ph                                                      3-88 4 CO N(Ac) 2,4-diMe--Ph                                                  3-89 4 CO N(Ac) 3,4-diMe--Ph                                                  3-90 4 CO N(Ac) 2-(CF.sub.3)Ph                                                3-91 4 CO N(Ac) 4-(CF.sub.3)Ph                                                3-92 4 CO N(Ac) 2-MeOPh                                                       3-93 4 CO N(Ac) 4-MeOPh                                                       3-94 4 CO N(Ac) 2-EtOPh                                                       3-95 4 CO N(Ac) 4-EtOPh                                                       3-96 4 CO N(Ac) 2-HOPh                                                        3-97 4 CO N(Ac) 4-HOPh                                                        3-98 4 CO N(Ac) 2-(HOOC)Ph                                                    3-99 4 CO N(Ac) 4-(HOOC)Ph                                                    3-100 4 CO N(Ac) 2-(MeOOC)Ph                                                  3-101 4 CO N(Ac) 4-(MeOOC)Ph                                                  3-102 4 CO N(Ac) 2-(EtOOC)Ph                                                  3-103 4 CO N(Ac) 4-(EtOOC)Ph                                                  3-104 4 CO N(Ac) 2-(tBuOOC)Ph                                                 3-105 4 CO N(Ac) 4-(tBuOOC)Ph                                                 3-106 4 CO N(Ac) 2-Cl--Ph                                                     3-107 4 CO N(Ac) 4-Cl--Ph                                                     3-108 4 CO N(Ac) 2-Br--Ph                                                     3-109 4 CO N(Ac) 4-Br--Ph                                                     3-110 4 CO N(Ac) 2-I--Ph                                                      3-111 4 CO N(Ac) 4-I--Ph                                                      3-112 4 CO N(Ac) 2-NO.sub.2 --Ph                                              3-113 4 CO N(Ac) 4-NO.sub.2 --Ph                                              3-114 4 CO N(Ac) 2-NH.sub.2 --Ph                                              3-115 4 CO N(Ac) 4-NH.sub.2 --Ph                                              3-116 4 CO N(Ac) 2-(HO.sub.3 S)Ph                                             3-117 4 CO N(Ac) 4-(HO.sub.3 S)Ph                                             3-118 4 CO N(Ac) 2-(NH.sub.2 O.sub.2 S)Ph                                     3-119 4 CO N(Ac) 4-(NH.sub.2 O.sub.2 S)Ph                                     3-120 4 CO N(Ac) 2-CN--Ph                                                     3-121 4 CO N(Ac) 4-CN--Ph                                                     3-122 4 CO N(Ac) 2-(HOCH.sub.2)Ph                                             3-123 4 CO N(Ac) 4-(HOCH.sub.2)Ph                                             3-124 4 CO N(Ac) Me                                                           3-125 4 CO N(Ac) Et                                                           3-126 4 CO N(Ac) Pr                                                           3-127 4 CO N(Ac) iPr                                                          3-128 4 CO N(Ac) Bu                                                           3-129 4 CO N(Ac) HOOCCH.sub.2 --                                              3-130 4 CO N(Ac) MeOOCCH.sub.2 --                                             3-131 4 CO N(Ac) MeCH(COOH)                                                   3-132 4 CO N(Ac) HOOC--(CH.sub.2).sub.2 --                                    3-133 4 CO N(Ac) MeCH(COOMe)                                                  3-134 4 CO N(Ac) 1-HOOC-iBu                                                   3-135 4 CO N(Ac) 1-MeOOC-iBu                                                  3-136 4 CO N(Ac) 1-HOOC-iPn                                                   3-137 4 CO N(Ac) 1-MeOOC-iPn                                                  3-138 4 CO N(Ac) 1-HOOC-2-Me--Bu                                              3-139 4 CO N(Ac) 1-MeOOC-2-Me--Bu                                             3-140 4 CO N(Ac) CH.sub.2 CH.sub.2 SO.sub.3 H                                 3-141 4 CO N(Ac) OH                                                           3-142 4 CO N(Ac) MeO                                                          3-143 4 CO N(Ac) EtO                                                          3-144 4 CO N(Ac) PrO                                                          3-145 4 CO N(Ac) iPrO                                                         3-146 4 CO N(Ac) BuO                                                          3-147 4 CO N(Ac) iBuO                                                         3-148 4 CO N(Ac) sBuO                                                         3-149 4 CO N(Ac) tBuO                                                         3-150 4 CO N(Ac) HxO                                                          3-151 4 CO N(Ac) PhO                                                          3-152 4 CO N(Ac) BnO                                                          3-153 4 CO N(Ac) Z-1                                                          3-154 4 CO N(Ac) Z-2                                                          3-155 4 CO N(Ac) Z-3                                                          3-156 4 CO N(Ac) Z-4                                                          3-157 4 CO N(Ac) Z-5                                                          3-158 4 CO N(Ac) Z-6                                                          3-159 4 CO N(Ac) Z-7                                                          3-160 4 CO N(Ac) Z-8                                                          3-161 4 CO N(Ac) Z-9                                                          3-162 4 CO N(Ac) Z-10                                                         3-163 4 CO N(Ac) Z-11                                                         3-164 4 CO N(Ac) Z-12                                                         3-165 4 CO N(Ac) 3-Py                                                         3-166 4 CO N(Ac) 4-Py                                                         3-167 4 COO -- H                                                              3-168 4 COO -- Ph                                                             3-169 4 COO -- 2-Me--Ph                                                       3-170 4 COO -- 4-Me--Ph                                                       3-171 4 COO -- 2,4-diMe--Ph                                                   3-172 4 COO -- 3,4-diMe--Ph                                                   3-173 4 COO -- 2-(CF.sub.3)Ph                                                 3-174 4 COO -- 4-(CF.sub.3)Ph                                                 3-175 4 COO -- 2-MeOPh                                                        3-176 4 COO -- 4-MeOPh                                                        3-177 4 COO -- 2-EtOPh                                                        3-178 4 COO -- 4-EtOPh                                                        3-179 4 COO -- 2-HOPh                                                         3-180 4 COO -- 4-HOPh                                                         3-181 4 COO -- 2-(HOOC)Ph                                                     3-182 4 COO -- 4-(HOOC)Ph                                                     3-183 4 COO -- 2-(MeOOC)Ph                                                    3-184 4 COO -- 4-(MeOOC)Ph                                                    3-185 4 COO -- 2-(EtOOC)Ph                                                    3-186 4 COO -- 4-(EtOOC)Ph                                                    3-187 4 COO -- 2-(tBuOOC)Ph                                                   3-188 4 COO -- 4-(tBuOOC)Ph                                                   3-189 4 COO -- 2-Cl--Ph                                                       3-190 4 COO -- 4-Cl--Ph                                                       3-191 4 COO -- 2-Br--Ph                                                       3-192 4 COO -- 4-Br--Ph                                                       3-193 4 COO -- 2-I--Ph                                                        3-194 4 COO -- 4-I--Ph                                                        3-195 4 COO -- 2-NO.sub.2 --Ph                                                3-196 4 COO -- 4-NO.sub.2 --Ph                                                3-197 4 COO -- 2-NH.sub.2 --Ph                                                3-198 4 COO -- 4-NH.sub.2 --Ph                                                3-199 4 COO -- 2-(HO.sub.3 S)Ph                                               3-200 4 COO -- 4-(HO.sub.3 S)Ph                                               3-201 4 COO -- 2-(NH.sub.2 O.sub.2 S)Ph                                       3-202 4 COO -- 4-(NH.sub.2 O.sub.2 S)Ph                                       3-203 4 COO -- 2-CN--Ph                                                       3-204 4 COO -- 4-CN--Ph                                                       3-205 4 COO -- 2-(HOCH.sub.2)Ph                                               3-206 4 COO -- 4-(HOCH.sub.2)Ph                                               3-207 4 COO -- Me                                                             3-208 4 COO -- Et                                                             3-209 4 COO -- Pr                                                             3-210 4 COO -- iPr                                                            3-211 4 COO -- Bu                                                             3-212 4 COO -- HOOCCH.sub.2 --                                                3-213 4 COO -- HOOC--(CH.sub.2).sub.2 --                                      3-214 4 COO -- MeCH(COOMe)                                                    3-215 4 COO -- 1-HOOC-iBu                                                     3-216 4 COO -- 1-HOOC-iPn                                                     3-217 4 COO -- Z-1                                                            3-218 4 COO -- Z-2                                                            3-219 4 COO -- Z-3                                                            3-220 4 COO -- Z-4                                                            3-221 4 COO -- Z-5                                                            3-222 4 COO -- Z-6                                                            3-223 4 COO -- Z-7                                                            3-224 4 COO -- Z-8                                                            3-225 4 COO -- Z-9                                                            3-226 4 COO -- Z-10                                                           3-227 4 COO -- Z-11                                                           3-228 4 COO -- Z-12                                                           3-229 4 COO -- 3-Py                                                           3-230 4 COO -- 4-Py                                                           3-231 4 CONHCO -- H                                                           3-232 4 CONHCO -- Ph                                                          3-233 4 CONHCO -- 2-Me--Ph                                                    3-234 4 CONHCO -- 4-Me--Ph                                                    3-235 4 CONHCO -- 2,4-diMe--Ph                                                3-236 4 CONHCO -- 3,4-diMe--Ph                                                3-237 4 CONHCO -- 2-(CF.sub.3)Ph                                              3-238 4 CONHCO -- 4-(CF.sub.3)Ph                                              3-239 4 CONHCO -- 2-MeOPh                                                     3-240 4 CONHCO -- 4-MeOPh                                                     3-241 4 CONHCO -- 2-EtOPh                                                     3-242 4 CONHCO -- 4-EtOPh                                                     3-243 4 CONHCO -- 2-HOPh                                                      3-244 4 CONHCO -- 4-HOPh                                                      3-245 4 CONHCO -- 2-(HOOC)Ph                                                  3-246 4 CONHCO -- 4-(HOOC)Ph                                                  3-247 4 CONHCO -- 2-(MeOOC)Ph                                                 3-248 4 CONHCO -- 4-(MeOOC)Ph                                                 3-249 4 CONHCO -- 2-(EtOOC)Ph                                                 3-250 4 CONHCO -- 4-(EtOOC)Ph                                                 3-251 4 CONHCO -- 2-(tBuOOC)Ph                                                3-252 4 CONHCO -- 4-(tBuOOC)Ph                                                3-253 4 CONHCO -- 2-Cl--Ph                                                    3-254 4 CONHCO -- 4-Cl--Ph                                                    3-255 4 CONHCO -- 2-Br--Ph                                                    3-256 4 CONHCO -- 4-Br--Ph                                                    3-257 4 CONHCO -- 2-I--Ph                                                     3-258 4 CONHCO -- 4-I--Ph                                                     3-259 4 CONHCO -- 2-NO.sub.2 --Ph                                             3-260 4 CONHCO -- 4-NO.sub.2 --Ph                                             3-261 4 CONHCO -- 2-NH.sub.2 --Ph                                             3-262 4 CONHCO -- 4-NH.sub.2 --Ph                                             3-263 4 CONHCO -- 2-(HO.sub.3 S)Ph                                            3-264 4 CONHCO -- 4-(HO.sub.3 S)Ph                                            3-265 4 CONHCO -- 2-(NH.sub.2 O.sub.2 S)Ph                                    3-266 4 CONHCO -- 4-(NH.sub.2 O.sub.2 S)Ph                                    3-267 4 CONHCO -- 2-CN--Ph                                                    3-268 4 CONHCO -- 4-CN--Ph                                                    3-269 4 CONHCO -- 2-(HOCH.sub.2)Ph                                            3-270 4 CONHCO -- 4-(HOCH.sub.2)Ph                                            3-271 4 CONHCO -- Me                                                          3-272 4 CONHCO -- Et                                                          3-273 4 CONHCO -- Pr                                                          3-274 4 CONHCO -- iPr                                                         3-275 4 CONHCO -- Bu                                                          3-276 4 CONHCO -- HOOCCH.sub.2 --                                             3-277 4 CONHCO -- MeOOCCH.sub.2 --                                            3-278 4 CONHCO -- MeCH(COOH)                                                  3-279 4 CONHCO -- HOOC--(CH.sub.2).sub.2 --                                   3-280 4 CONHCO -- MeCH(COOMe)                                                 3-281 4 CONHCO -- 1-HOOC-iBu                                                  3-282 4 CONHCO -- 1-MeOOC-iBu                                                 3-283 4 CONHCO -- 1-HOOC-iPn                                                  3-284 4 CONHCO -- 1-MeOOC-iPn                                                 3-285 4 CONHCO -- 1-HOOC-2-Me--Bu                                             3-286 4 CONHCO -- 1-MeOOC-2-Me--Bu                                            3-287 4 CONHCO -- CH.sub.2 CH.sub.2 SO.sub.3 H                                3-288 4 CONHCO -- Z-1                                                         3-289 4 CONHCO -- Z-2                                                         3-290 4 CONHCO -- Z-3                                                         3-291 4 CONHCO -- Z-4                                                         3-292 4 CONHCO -- Z-5                                                         3-293 4 CONHCO -- Z-6                                                         3-294 4 CONHCO -- Z-7                                                         3-295 4 CONHCO -- Z-8                                                         3-296 4 CONHCO -- Z-9                                                         3-297 4 CONHCO -- Z-10                                                        3-298 4 CONHCO -- Z-11                                                        3-299 4 CONHCO -- Z-12                                                        3-300 4 CONHCO -- 3-Py                                                        3-301 4 CONHCO -- 4-Py                                                        3-302 4 CON(Ac)CO -- H                                                        3-303 4 CON(Ac)CO -- Ph                                                       3-304 4 CON(Ac)CO -- 2-Me--Ph                                                 3-305 4 CON(Ac)CO -- 4-Me--Ph                                                 3-306 4 CON(Ac)CO -- 2,4-diMe--Ph                                             3-307 4 CON(Ac)CO -- 3,4-diMe--Ph                                             3-308 4 CON(Ac)CO -- 2-(CF.sub.3)Ph                                           3-309 4 CON(Ac)CO -- 4-(CF.sub.3)Ph                                           3-310 4 CON(Ac)CO -- 2-MeOPh                                                  3-311 4 CON(Ac)CO -- 4-MeOPh                                                  3-312 4 CON(Ac)CO -- 2-EtOPh                                                  3-313 4 CON(Ac)CO -- 4-EtOPh                                                  3-314 4 CON(Ac)CO -- 2-HOPh                                                   3-315 4 CON(Ac)CO -- 4-HOPh                                                   3-316 4 CON(Ac)CO -- 2-(HOOC)Ph                                               3-317 4 CON(Ac)CO -- 4-(HOOC)Ph                                               3-318 4 CON(Ac)CO -- 2-(MeOOC)Ph                                              3-319 4 CON(Ac)CO -- 4-(MeOOC)Ph                                              3-320 4 CON(Ac)CO -- 2-(EtOOC)Ph                                              3-321 4 CON(Ac)CO -- 4-(EtOOC)Ph                                              3-322 4 CON(Ac)CO -- 2-(tBuOOC)Ph                                             3-323 4 CON(Ac)CO -- 4-(tBuOOC)Ph                                             3-324 4 CON(Ac)CO -- 2-Cl--Ph                                                 3-325 4 CON(Ac)CO -- 4-Cl--Ph                                                 3-326 4 CON(Ac)CO -- 2-Br--Ph                                                 3-327 4 CON(Ac)CO -- 4-Br--Ph                                                 3-328 4 CON(Ac)CO -- 2-I--Ph                                                  3-329 4 CON(Ac)CO -- 4-I--Ph                                                  3-330 4 CON(Ac)CO -- 2-NO.sub.2 --Ph                                          3-331 4 CON(Ac)CO -- 4-NO.sub.2 --Ph                                          3-332 4 CON(Ac)CO -- 2-NH.sub.2 --Ph                                          3-333 4 CON(Ac)CO -- 4-NH.sub.2 --Ph                                          3-334 4 CON(Ac)CO -- 2-(HO.sub.3 S)Ph                                         3-335 4 CON(Ac)CO -- 4-(HO.sub.3 S)Ph                                         3-336 4 CON(Ac)CO -- 2-(NH.sub.2 O.sub.2 S)Ph                                 3-337 4 CON(Ac)CO -- 4-(NH.sub.2 O.sub.2 S)Ph                                 3-338 4 CON(Ac)CO -- 2-CN--Ph                                                 3-339 4 CON(Ac)CO -- 4-CN--Ph                                                 3-340 4 CON(Ac)CO -- 2-(HOCH.sub.2)Ph                                         3-341 4 CON(Ac)CO -- 4-(HOCH.sub.2)Ph                                         3-342 4 CON(Ac)CO -- Me                                                       3-343 4 CON(Ac)CO -- Et                                                       3-344 4 CON(Ac)CO -- Pr                                                       3-345 4 CON(Ac)CO -- iPr                                                      3-346 4 CON(Ac)CO -- Bu                                                       3-347 4 CON(Ac)CO -- HOOCCH.sub.2 --                                          3-348 4 CON(Ac)CO -- MeOOCCH.sub.2 --                                         3-349 4 CON(Ac)CO -- MeCH(COOH)                                               3-350 4 CON(Ac)CO -- HOOC--(CH.sub.2).sub.2 --                                3-351 4 CON(Ac)CO -- MeCH(COOMe)                                              3-352 4 CON(Ac)CO -- 1-HOOC-iBu                                               3-353 4 CON(Ac)CO -- 1-MeOOC-iBu                                              3-354 4 CON(Ac)CO -- 1-HOOC-iPn                                               3-355 4 CON(Ac)CO -- 1-MeOOC-iPn                                              3-356 4 CON(Ac)CO -- 1-HOOC-2-Me--Bu                                          3-357 4 CON(Ac)CO -- 1-MeOOC-2-Me--Bu                                         3-358 4 CON(Ac)CO -- CH.sub.2 CH.sub.2 SO.sub.3 H                             3-359 4 CON(Ac)CO -- Z-1                                                      3-360 4 CON(Ac)CO -- Z-2                                                      3-361 4 CON(Ac)CO -- Z-3                                                      3-362 4 CON(Ac)CO -- Z-4                                                      3-363 4 CON(Ac)CO -- Z-5                                                      3-364 4 CON(Ac)CO -- Z-6                                                      3-365 4 CON(Ac)CO -- Z-7                                                      3-366 4 CON(Ac)CO -- Z-8                                                      3-367 4 CON(Ac)CO -- Z-9                                                      3-368 4 CON(Ac)CO -- Z-10                                                     3-369 4 CON(Ac)CO -- Z-11                                                     3-370 4 CON(Ac)CO -- Z-12                                                     3-371 4 CON(Ac)CO -- 3-Py                                                     3-372 4 CON(Ac)CO -- 4-Py                                                     3-373 4 CONHCO NH H                                                           3-374 4 CONHCO NH Ph                                                          3-375 4 CONHCO NH 2-Me--Ph                                                    3-376 4 CONHCO NH 4-Me--Ph                                                    3-377 4 CONHCO NH 2,4-diMe--Ph                                                3-378 4 CONHCO NH 3,4-diMe--Ph                                                3-379 4 CONHCO NH 2-(CF.sub.3)Ph                                              3-380 4 CONHCO NH 4-(CF.sub.3)Ph                                              3-381 4 CONHCO NH 2-MeOPh                                                     3-382 4 CONHCO NH 4-MeOPh                                                     3-383 4 CONHCO NH 2-EtOPh                                                     3-384 4 CONHCO NH 4-EtOPh                                                     3-385 4 CONHCO NH 2-HOPh                                                      3-386 4 CONHCO NH 4-HOPh                                                      3-387 4 CONHCO NH 2-(HOOC)Ph                                                  3-388 4 CONHCO NH 4-(HOOC)Ph                                                  3-389 4 CONHCO NH 2-(MeOOC)Ph                                                 3-390 4 CONHCO NH 4-(MeOOC)Ph                                                 3-391 4 CONHCO NH 2-(EtOOC)Ph                                                 3-392 4 CONHCO NH 4-(EtOOC)Ph                                                 3-393 4 CONHCO NH 2-(tBuOOC)Ph                                                3-394 4 CONHCO NH 4-(tBuOOC)Ph                                                3-395 4 CONHCO NH 2-Cl--Ph                                                    3-396 4 CONHCO NH 4-Cl--Ph                                                    3-397 4 CONHCO NH 2-Br--Ph                                                    3-398 4 CONHCO NH 4-Br--Ph                                                    3-399 4 CONHCO NH 2-I--Ph                                                     3-400 4 CONHCO NH 4-I--Ph                                                     3-401 4 CONHCO NH 2-NO.sub.2 --Ph                                             3-402 4 CONHCO NH 4-NO.sub.2 --Ph                                             3-403 4 CONHCO NH 2-NH.sub.2 --Ph                                             3-404 4 CONHCO NH 4-NH.sub.2 --Ph                                             3-405 4 CONHCO NH 2-(HO.sub.3 S)Ph                                            3-406 4 CONHCO NH 4-(HO.sub.3 S)Ph                                            3-407 4 CONHCO NH 2-(NH.sub.2 O.sub.2 S)Ph                                    3-408 4 CONHCO NH 4-(NH.sub.2 O.sub.2 S)Ph                                    3-409 4 CONHCO NH 2-CN--Ph                                                    3-410 4 CONHCO NH 4-CN--Ph                                                    3-411 4 CONHCO NH 2-(HOCH.sub.2)Ph                                            3-412 4 CONHCO NH 4-(HOCH.sub.2)Ph                                            3-413 4 CONHCO NH Me                                                          3-414 4 CONHCO NH Et                                                          3-415 4 CONHCO NH Pr                                                          3-416 4 CONHCO NH iPr                                                         3-417 4 CONHCO NH Bu                                                          3-418 4 CONHCO NH HOOCCH.sub.2 --                                             3-419 4 CONHCO NH MeOOCCH.sub.2 --                                            3-420 4 CONHCO NH MeCH(COOH)                                                  3-421 4 CONHCO NH HOOC--(CH.sub.2).sub.2 --                                   3-422 4 CONHCO NH MeCH(COOMe)                                                 3-423 4 CONHCO NH 1-HOOC-iBu                                                  3-424 4 CONHCO NH 1-MeOOC-iBu                                                 3-425 4 CONHCO NH 1-HOOC-iPn                                                  3-426 4 CONHCO NH 1-MeOOC-iPn                                                 3-427 4 CONHCO NH 1-HOOC-2-Me--Bu                                             3-428 4 CONHCO NH 1-MeOOC-2-Me--Bu                                            3-429 4 CONHCO NH CH.sub.2 CH.sub.2 SO.sub.3 H                                3-430 4 CONHCO NH HO                                                          3-431 4 CONHCO NH MeO                                                         3-432 4 CONHCO NH EtO                                                         3-433 4 CONHCO NH PrO                                                         3-434 4 CONHCO NH iPrO                                                        3-435 4 CONHCO NH BuO                                                         3-436 4 CONHCO NH iBuO                                                        3-437 4 CONHCO NH sBuO                                                        3-438 4 CONHCO NH tBuO                                                        3-439 4 CONHCO NH HxO                                                         3-440 4 CONHCO NH PhO                                                         3-441 4 CONHCO NH BnO                                                         3-442 4 CONHCO NH Z-1                                                         3-443 4 CONHCO NH Z-2                                                         3-444 4 CONHCO NH Z-3                                                         3-445 4 CONHCO NH Z-4                                                         3-446 4 CONHCO NH Z-5                                                         3-447 4 CONHCO NH Z-6                                                         3-448 4 CONHCO NH Z-7                                                         3-449 4 CONHCO NH Z-8                                                         3-450 4 CONHCO NH Z-9                                                         3-451 4 CONHCO NH Z-10                                                        3-452 4 CONHCO NH Z-11                                                        3-453 4 CONHCO NH Z-12                                                        3-454 4 CONHCO NH 3-Py                                                        3-455 4 CONHCO NH 4-Py                                                        3-456 4 CONHSO.sub.2 -- H                                                     3-457 4 CONHSO.sub.2 -- Ph                                                    3-458 4 CONHSO.sub.2 -- 2-Me--Ph                                              3-459 4 CONHSO.sub.2 -- 4-Me--Ph                                              3-460 4 CONHSO.sub.2 -- 2,4-diMe--Ph                                          3-461 4 CONHSO.sub.2 -- 3,4-diMe--Ph                                          3-462 4 CONHSO.sub.2 -- 2-(CF.sub.3)Ph                                        3-463 4 CONHSO.sub.2 -- 4-(CF.sub.3)Ph                                        3-464 4 CONHSO.sub.2 -- 2-MeOPh                                               3-465 4 CONHSO.sub.2 -- 4-MeOPh                                               3-466 4 CONHSO.sub.2 -- 2-EtOPh                                               3-467 4 CONHSO.sub.2 -- 4-EtOPh                                               3-468 4 CONHSO.sub.2 -- 2-HOPh                                                3-469 4 CONHSO.sub.2 -- 4-HOPh                                                3-470 4 CONHSO.sub.2 -- 2-(HOOC)Ph                                            3-471 4 CONHSO.sub.2 -- 4-(HOOC)Ph                                            3-472 4 CONHSO.sub.2 -- 2-(MeOOC)Ph                                           3-473 4 CONHSO.sub.2 -- 4-(MeOOC)Ph                                           3-474 4 CONHSO.sub.2 -- 2-(EtOOC)Ph                                           3-475 4 CONHSO.sub.2 -- 4-(EtOOC)Ph                                           3-476 4 CONHSO.sub.2 -- 2-(tBuOOC)Ph                                          3-477 4 CONHSO.sub.2 -- 4-(tBuOOC)Ph                                          3-478 4 CONHSO.sub.2 -- 2-Cl--Ph                                              3-479 4 CONHSO.sub.2 -- 4-Cl--Ph                                              3-480 4 CONHSO.sub.2 -- 2-Br--Ph                                              3-481 4 CONHSO.sub.2 -- 4-Br--Ph                                              3-482 4 CONHSO.sub.2 -- 2-I--Ph                                               3-483 4 CONHSO.sub.2 -- 4-I--Ph                                               3-484 4 CONHSO.sub.2 -- 2-NO.sub.2 --Ph                                       3-485 4 CONHSO.sub.2 -- 4-NO.sub.2 --Ph                                       3-486 4 CONHSO.sub.2 -- 2-NH.sub.2 --Ph                                       3-487 4 CONHSO.sub.2 -- 4-NH.sub.2 --Ph                                       3-488 4 CONHSO.sub.2 -- 2-(HO.sub.3 S)Ph                                      3-489 4 CONHSO.sub.2 -- 4-(HO.sub.3 S)Ph                                      3-490 4 CONHSO.sub.2 -- 2-(NH.sub.2 O.sub.2 S)Ph                              3-491 4 CONHSO.sub.2 -- 4-(NH.sub.2 O.sub.2 S)Ph                              3-492 4 CONHSO.sub.2 -- 2-CN--Ph                                              3-493 4 CONHSO.sub.2 -- 4-CN--Ph                                              3-494 4 CONHSO.sub.2 -- 2-(HOCH.sub.2)Ph                                      3-495 4 CONHSO.sub.2 -- 4-(HOCH.sub.2)Ph                                      3-496 4 CONHSO.sub.2 -- Me                                                    3-497 4 CONHSO.sub.2 -- Et                                                    3-498 4 CONHSO.sub.2 -- Pr                                                    3-499 4 CONHSO.sub.2 -- iPr                                                   3-500 4 CONHSO.sub.2 -- Bu                                                    3-501 4 CONHSO.sub.2 -- HOOCCH.sub.2 --                                       3-502 4 CONHSO.sub.2 -- MeOOCCH.sub.2 --                                      3-503 4 CONHSO.sub.2 -- MeCH(COOH)                                            3-504 4 CONHSO.sub.2 -- HOOC-(CH.sub.2).sub.2 --                              3-505 4 CONHSO.sub.2 -- MeCH(COOMe)                                           3-506 4 CONHSO.sub.2 -- 1-HOOC-iBu                                            3-507 4 CONHSO.sub.2 -- 1-MeOOC-iBu                                           3-508 4 CONHSO.sub.2 -- 1-HOOC-iPn                                            3-509 4 CONHSO.sub.2 -- 1-MeOOC-iPn                                           3-510 4 CONHSO.sub.2 -- 1-HOOC-2-Me--Bu                                       3-511 4 CONHSO.sub.2 -- 1-MeOOC-2-Me--Bu                                      3-512 4 CONHSO.sub.2 -- CH.sub.2 CH.sub.2 SO.sub.3 H                          3-513 4 CONHSO.sub.2 -- OH                                                    3-514 4 CONHSO.sub.2 -- MeO                                                   3-515 4 CONHSO.sub.2 -- EtO                                                   3-516 4 CONHSO.sub.2 -- Pro                                                   3-517 4 CONHSO.sub.2 -- iPrO                                                  3-518 4 CONHSO.sub.2 -- BuO                                                   3-519 4 CONHSO.sub.2 -- iBuO                                                  3-520 4 CONHSO.sub.2 -- sBuO                                                  3-521 4 CONHSO.sub.2 -- tBuO                                                  3-522 4 CONHSO.sub.2 -- HxO                                                   3-523 4 CONHSO.sub.2 -- PhO                                                   3-524 4 CONHSO.sub.2 -- BnO                                                   3-525 4 CONHSO.sub.2 -- Z-1                                                   3-526 4 CONHSO.sub.2 -- Z-2                                                   3-527 4 CONHSO.sub.2 -- Z-3                                                   3-528 4 CONHSO.sub.2 -- Z-4                                                   3-529 4 CONHSO.sub.2 -- Z-5                                                   3-530 4 CONHSO.sub.2 -- Z-6                                                   3-531 4 CONHSO.sub.2 -- Z-7                                                   3-532 4 CONHSO.sub.2 -- Z-8                                                   3-533 4 CONHSO.sub.2 -- Z-9                                                   3-534 4 CONHSO.sub.2 -- Z-10                                                  3-535 4 CONHSO.sub.2 -- Z-11                                                  3-536 4 CONHSO.sub.2 -- Z-12                                                  3-537 4 CONHSO.sub.2 -- 3-Py                                                  3-538 4 CONHSO.sub.2 -- 4-Py                                                  3-539 4 CONHSO.sub.2 NH H                                                     3-540 4 CONHSO.sub.2 NH Ph                                                    3-541 4 CONHSO.sub.2 NH 2-Me--Ph                                              3-542 4 CONHSO.sub.2 NH 4-Me--Ph                                              3-543 4 CONHSO.sub.2 NH 2,4-diMe--Ph                                          3-544 4 CONHSO.sub.2 NH 3,4-diMe--Ph                                          3-545 4 CONHSO.sub.2 NH 2-(CF.sub.3)Ph                                        3-546 4 CONHSO.sub.2 NH 4-(CF.sub.3)Ph                                        3-547 4 CONHSO.sub.2 NH 2-MeOPh                                               3-548 4 CONHSO.sub.2 NH 4-MeOPh                                               3-549 4 CONHSO.sub.2 NH 2-EtOPh                                               3-550 4 CONHSO.sub.2 NH 4-EtOPh                                               3-551 4 CONHSO.sub.2 NH 2-HOPh                                                3-552 4 CONHSO.sub.2 NH 4-HOPh                                                3-553 4 CONHSO.sub.2 NH 2-(HOOC)Ph                                            3-554 4 CONHSO.sub.2 NH 4-(HOOC)Ph                                            3-555 4 CONHSO.sub.2 NH 2-(MeOOC)Ph                                           3-556 4 CONHSO.sub.2 NH 4-(MeOOC)Ph                                           3-557 4 CONHSO.sub.2 NH 2-(EtOOC)Ph                                           3-558 4 CONHSO.sub.2 NH 4-(EtOOC)Ph                                           3-559 4 CONHSO.sub.2 NH 2-(tBuOOC)Ph                                          3-560 4 CONHSO.sub.2 NH 4-(tBuOOC)Ph                                          3-561 4 CONHSO.sub.2 NH 2-Cl--Ph                                              3-562 4 CONHSO.sub.2 NH 4-Cl--Ph                                              3-563 4 CONHSO.sub.2 NH 2-Br--Ph                                              3-564 4 CONHSO.sub.2 NH 4-Br--Ph                                              3-565 4 CONHSO.sub.2 NH 2-I--Ph                                               3-566 4 CONHSO.sub.2 NH 4-I--Ph                                               3-567 4 CONHSO.sub.2 NH 2-NO.sub.2 --Ph                                       3-568 4 CONHSO.sub.2 NH 4-NO.sub.2 --Ph                                       3-569 4 CONHSO.sub.2 NH 2-NH.sub.2 --Ph                                       3-570 4 CONHSO.sub.2 NH 4-NH.sub.2 --Ph                                       3-571 4 CONHSO.sub.2 NH 2-(HO.sub.3 S)Ph                                      3-572 4 CONHSO.sub.2 NH 4-(HO.sub.3 S)Ph                                      3-573 4 CONHSO.sub.2 NH 2-(NH.sub.2 O.sub.2 S)Ph                              3-574 4 CONHSO.sub.2 NH 4-(NH.sub.2 O.sub.2 S)Ph                              3-575 4 CONHSO.sub.2 NH 2-CN--Ph                                              3-576 4 CONHSO.sub.2 NH 4-CN--Ph                                              3-577 4 CONHSO.sub.2 NH 2-(HOCH.sub.2)Ph                                      3-578 4 CONHSO.sub.2 NH 4-(HOCH.sub.2)Ph                                      3-579 4 CONHSO.sub.2 NH Me                                                    3-580 4 CONHSO.sub.2 NH Et                                                    3-581 4 CONHSO.sub.2 NH Pr                                                    3-582 4 CONHSO.sub.2 NH iPr                                                   3-583 4 CONHSO.sub.2 NH Bu                                                    3-584 4 CONHSO.sub.2 NH HOOCCH.sub.2 --                                       3-585 4 CONHSO.sub.2 NH MeOOCCH.sub.2 --                                      3-586 4 CONHSO.sub.2 NH MeCH(COOH)                                            3-587 4 CONHSO.sub.2 NH HOOC--(CH.sub.2).sub.2 --                             3-588 4 CONHSO.sub.2 NH MeCH(COOMe)                                           3-589 4 CONHSO.sub.2 NH 1-HOOC-iBu                                            3-590 4 CONHSO.sub.2 NH 1-MeOOC-iBu                                           3-591 4 CONHSO.sub.2 NH 1-HOOC-iPn                                            3-592 4 CONHSO.sub.2 NH 1-MeOOC-iPn                                           3-593 4 CONHSO.sub.2 NH 1-HOOC-2-Me--Bu                                       3-594 4 CONHSO.sub.2 NH 1-MeOOC-2-Me--Bu                                      3-595 4 CONHSO.sub.2 NH CH.sub.2 CH.sub.2 SO.sub.3 H                          3-596 4 CONHSO.sub.2 NH OH                                                    3-597 4 CONHSO.sub.2 NH MeO                                                   3-598 4 CONHSO.sub.2 NH EtO                                                   3-599 4 CONHSO.sub.2 NH PrO                                                   3-600 4 CONHSO.sub.2 NH iPro                                                  3-601 4 CONHSO.sub.2 NH BuO                                                   3-602 4 CONHSO.sub.2 NH iBuO                                                  3-603 4 CONHSO.sub.2 NH sBuO                                                  3-604 4 CONHSO.sub.2 NH tBuO                                                  3-605 4 CONHSO.sub.2 NH HxO                                                   3-606 4 CONHSO.sub.2 NH PhO                                                   3-607 4 CONHSO.sub.2 NH BnO                                                   3-608 4 CONHSO.sub.2 NH Z-1                                                   3-609 4 CONHSO.sub.2 NH Z-2                                                   3-610 4 CONHSO.sub.2 NH Z-3                                                   3-611 4 CONHSO.sub.2 NH Z-4                                                   3-612 4 CONHSO.sub.2 NH Z-5                                                   3-613 4 CONHSO.sub.2 NH Z-6                                                   3-614 4 CONHSO.sub.2 NH Z-7                                                   3-615 4 CONHSO.sub.2 NH Z-8                                                   3-616 4 CONHSO.sub.2 NH Z-9                                                   3-617 4 CONHSO.sub.2 NH Z-10                                                  3-618 4 CONHSO.sub.2 NH Z-11                                                  3-619 4 CONHSO.sub.2 NH Z-12                                                  3-620 4 CONHSO.sub.2 NH 3-Py                                                  3-621 4 CONHSO.sub.2 NH 4-Py                                                  3-622 4 NHCO -- H                                                             3-623 4 NHCO -- Ph                                                            3-624 4 NHCO -- 2-Me--Ph                                                      3-625 4 NHCO -- 4-Me--Ph                                                      3-626 4 NHCO -- 2,4-diMe--Ph                                                  3-627 4 NHCO -- 3,4-diMe--Ph                                                  3-628 4 NHCO -- 2-(CF.sub.3)Ph                                                3-629 4 NHCO -- 4-(CF.sub.3)Ph                                                3-630 4 NHCO -- 2-MeOPh                                                       3-631 4 NHCO -- 4-MeOPh                                                       3-632 4 NHCO -- 2-EtOPh                                                       3-633 4 NHCO -- 4-EtOPh                                                       3-634 4 NHCO -- 2-HOPh                                                        3-635 4 NHCO -- 4-HOPh                                                        3-636 4 NHCO -- 2-(HOOC)Ph                                                    3-637 4 NHCO -- 4-(HOOC)Ph                                                    3-638 4 NHCO -- 2-(MeOOC)Ph                                                   3-639 4 NHCO -- 4-(MeOOC)Ph                                                   3-640 4 NHCO -- 2-(EtOOC)Ph                                                   3-641 4 NHCO -- 4-(EtOOC)Ph                                                   3-642 4 NHCO -- 2-(tBuOOC)Ph                                                  3-643 4 NHCO -- 4-(tBuOOC)Ph                                                  3-644 4 NHCO -- 2-Cl--Ph                                                      3-645 4 NHCO -- 4-Cl--Ph                                                      3-646 4 NHCO -- 2-Br--Ph                                                      3-647 4 NHCO -- 4-Br--Ph                                                      3-648 4 NHCO -- 2-I--Ph                                                       3-649 4 NHCO -- 4-I--Ph                                                       3-650 4 NHCO -- 2-NO.sub.2 --Ph                                               3-651 4 NHCO -- 4-NO.sub.2 --Ph                                               3-652 4 NHCO -- 2-NH.sub.2 --Ph                                               3-653 4 NHCO -- 4-NH.sub.2 --Ph                                               3-654 4 NHCO -- 2-(HO.sub.3 S)Ph                                              3-655 4 NHCO -- 4-(HO.sub.3 S)Ph                                              3-656 4 NHCO -- 2-(NH.sub.2 O.sub.2 S)Ph                                      3-657 4 NHCO -- 4-(NH.sub.2 O.sub.2 S)Ph                                      3-658 4 NHCO -- 2-CN--Ph                                                      3-659 4 NHCO -- 4-CN--Ph                                                      3-660 4 NHCO -- 2-(HOCH.sub.2)Ph                                              3-661 4 NHCO -- 4-(HOCH.sub.2)Ph                                              3-662 4 NHCO -- Me                                                            3-663 4 NHCO -- Et                                                            3-664 4 NHCO -- Pr                                                            3-665 4 NHCO -- iPr                                                           3-666 4 NHCO -- Bu                                                            3-667 4 NHCO -- HOOCCH.sub.2 --                                               3-668 4 NHCO -- MeOOCCH.sub.2 --                                              3-669 4 NHCO -- MeCH(COOH)                                                    3-670 4 NHCO -- HOOC--(CH.sub.2).sub.2 --                                     3-671 4 NHCO -- MeCH(COOMe)                                                   3-672 4 NHCO -- 1-HOOC-iBu                                                    3-673 4 NHCO -- 1-HOOC-iPn                                                    3-674 4 NHCO -- 1-HOOC-2-Me-Bu                                                3-675 4 NHCO -- CH.sub.2 CH.sub.2 SO.sub.3 H                                  3-676 4 NHCO -- MeO                                                           3-677 4 NHCO -- EtO                                                           3-678 4 NHCO -- PrO                                                           3-679 4 NHCO -- Z-1                                                           3-680 4 NHCO -- Z-2                                                           3-681 4 NHCO -- Z-3                                                           3-682 4 NHCO -- Z-4                                                           3-683 4 NHCO -- Z-5                                                           3-684 4 NHCO -- Z-6                                                           3-685 4 NHCO -- Z-7                                                           3-686 4 NHCO -- Z-8                                                           3-687 4 NHCO -- Z-9                                                           3-688 4 NHCO -- Z-10                                                          3-689 4 NHCO -- Z-11                                                          3-690 4 NHCO -- Z-12                                                          3-691 4 NHCO -- 3-Py                                                          3-692 4 NHCO -- 4-Py                                                          3-693 4 NHCO NH H                                                             3-694 4 NHCO NH Ph                                                            3-695 4 NHCO NH 2-Me--Ph                                                      3-696 4 NHCO NH 4-Me--Ph                                                      3-697 4 NHCO NH 2,4-diMe--Ph                                                  3-698 4 NHCO NH 3,4-diMe--Ph                                                  3-699 4 NHCO NH 2-(CF.sub.3)Ph                                                3-700 4 NHCO NH 4-(CF.sub.3)Ph                                                3-701 4 NHCO NH 2-MeOPh                                                       3-702 4 NHCO NH 4-MeOPh                                                       3-703 4 NHCO NH 2-EtOPh                                                       3-704 4 NHCO NH 4-EtOPh                                                       3-705 4 NHCO NH 2-HOPh                                                        3-706 4 NHCO NH 4-HOPh                                                        3-707 4 NHCO NH 2-(HOOC)Ph                                                    3-708 4 NHCO NH 4-(HOOC)Ph                                                    3-709 4 NHCO NH 2-(MeOOC)Ph                                                   3-710 4 NHCO NH 4-(MeOOC)Ph                                                   3-711 4 NHCO NH 2-(EtOOC)Ph                                                   3-712 4 NHCO NH 4-(EtOOC)Ph                                                   3-713 4 NHCO NH 2-(tBuOOC)Ph                                                  3-714 4 NHCO NH 4-(tBuOOC)Ph                                                  3-715 4 NHCO NH 2-Cl--Ph                                                      3-716 4 NHCO NH 4-Cl--Ph                                                      3-717 4 NHCO NH 2-Br--Ph                                                      3-718 4 NHCO NH 4-Br--Ph                                                      3-719 4 NHCO NH 2-I--Ph                                                       3-720 4 NHCO NH 4-I--Ph                                                       3-721 4 NHCO NH 2-NO.sub.2 --Ph                                               3-722 4 NHCO NH 4-NO.sub.2 --Ph                                               3-723 4 NHCO NH 2-NH.sub.2 --Ph                                               3-724 4 NHCO NH 4-NH.sub.2 --Ph                                               3-725 4 NHCO NH 2-(HO.sub.3 S)Ph                                              3-726 4 NHCO NH 4-(HO.sub.3 S)Ph                                              3-727 4 NHCO NH 2-(NH.sub.2 O.sub.2 S)Ph                                      3-728 4 NHCO NH 4-(NH.sub.2 O.sub.2 S)Ph                                      3-729 4 NHCO NH 2-CN--Ph                                                      3-730 4 NHCO NH 4-CN--Ph                                                      3-731 4 NHCO NH 2-(HOCH.sub.2)Ph                                              3-732 4 NHCO NH 4-(HOCH.sub.2)Ph                                              3-733 4 NHCO NH Me                                                            3-734 4 NHCO NH Et                                                            3-735 4 NHCO NH Pr                                                            3-736 4 NHCO NH iPr                                                           3-737 4 NHCO NH Bu                                                            3-738 4 NHCO NH HOOCCH.sub.2 --                                               3-739 4 NHCO NH MeOOCCH.sub.2 --                                              3-740 4 NHCO NH MeCH(COOH)                                                    3-741 4 NHCO NH HOOC--(CH.sub.2).sub.2 --                                     3-742 4 NHCO NH MeCH(COOMe)                                                   3-743 4 NHCO NH 1-HOOC-iBu                                                    3-744 4 NHCO NH 1-MeOOC-iBu                                                   3-745 4 NHCO NH 1-HOOC-iPn                                                    3-746 4 NHCO NH 1-MeOOC-iPn                                                   3-747 4 NHCO NH 1-HOOC-2-Me--Bu                                               3-748 4 NHCO NH 1-MeOOC-2-Me--Bu                                              3-749 4 NHCO NH CH.sub.2 CH.sub.2 SO.sub.3 H                                  3-750 4 NHCO NH OH                                                            3-751 4 NHCO NH MeO                                                           3-752 4 NHCO NH EtO                                                           3-753 4 NHCO NH PrO                                                           3-754 4 NHCO NH iPro                                                          3-755 4 NHCO NH BuO                                                           3-756 4 NHCO NH iBuO                                                          3-757 4 NHCO NH sBuO                                                          3-758 4 NHCO NH tBuO                                                          3-759 4 NHCO NH HxO                                                           3-760 4 NHCO NH PhO                                                           3-761 4 NHCO NH BnO                                                           3-762 4 NHCO NH Z-1                                                           3-763 4 NHCO NH Z-2                                                           3-764 4 NHCO NH Z-3                                                           3-765 4 NHCO NH Z-4                                                           3-766 4 NHCO NH Z-5                                                           3-767 4 NHCO NH Z-6                                                           3-768 4 NHCO NH Z-7                                                           3-769 4 NHCO NH Z-8                                                           3-770 4 NHCO NH Z-9                                                           3-771 4 NHCO NH Z-10                                                          3-772 4 NHCO NH Z-11                                                          3-773 4 NHCO NH Z-12                                                          3-774 4 NHCO NH 3-Py                                                          3-775 4 NHCO NH 4-Py                                                          3-776 4 NHCO NMe Ph                                                           3-777 4 NHCO NMe 2-Me--Ph                                                     3-778 4 NHCO NMe 4-Me--Ph                                                     3-779 4 NHCO NMe 2,4-diMe--Ph                                                 3-780 4 NHCO NMe 3,4-diMe--Ph                                                 3-781 4 NHCO NMe 2-(CF.sub.3)Ph                                               3-782 4 NHCO NMe 4-(CF.sub.3)Ph                                               3-783 4 NHCO NMe 2-MeOPh                                                      3-784 4 NHCO NMe 4-MeOPh                                                      3-785 4 NHCO NMe 2-EtOPh                                                      3-786 4 NHCO NMe 4-EtOPh                                                      3-787 4 NHCO NMe 2-HOPh                                                       3-788 4 NHCO NMe 4-HOPh                                                       3-789 4 NHCO NMe 2-(HOOC)Ph                                                   3-790 4 NHCO NMe 4-(HOOC)Ph                                                   3-791 4 NHCO NMe 2-(MeOOC)Ph                                                  3-792 4 NHCO NMe 4-(MeOOC)Ph                                                  3-793 4 NHCO NMe 2-(EtOOC)Ph                                                  3-794 4 NHCO NMe 4-(EtOOC)Ph                                                  3-795 4 NHCO NMe 2-(tBuOOC)Ph                                                 3-796 4 NHCO NMe 4-(tBuOOC)Ph                                                 3-797 4 NHCO NMe 2-Cl--Ph                                                     3-798 4 NHCO NMe 4-Cl--Ph                                                     3-799 4 NHCO NMe 2-Br--Ph                                                     3-800 4 NHCO NMe 4-Br--Ph                                                     3-801 4 NHCO NMe 2-I--Ph                                                      3-802 4 NHCO NMe 4-I--Ph                                                      3-803 4 NHCO NMe 2-NO.sub.2 --Ph                                              3-804 4 NHCO NMe 4-NO.sub.2 --Ph                                              3-805 4 NHCO NMe 2-NH.sub.2 --Ph                                              3-806 4 NHCO NMe 4-NH.sub.2 --Ph                                              3-807 4 NHCO NMe 2-(HO.sub.3 S)Ph                                             3-808 4 NHCO NMe 4-(HO.sub.3 S)Ph                                             3-809 4 NHCO NMe 2-(NH.sub.2 O.sub.2 S)Ph                                     3-810 4 NHCO NMe 4-(NH.sub.2 O.sub.2 S)Ph                                     3-811 4 NHCO NMe 2-CN--Ph                                                     3-812 4 NHCO NMe 4-CN--Ph                                                     3-813 4 NHCO NMe 2-(HOCH.sub.2)Ph                                             3-814 4 NHCO NMe 4-(HOCH.sub.2)Ph                                             3-815 4 NHCO NMe Me                                                           3-816 4 NHCO NMe Et                                                           3-817 4 NHCO NMe Pr                                                           3-818 4 NHCO NMe iPr                                                          3-819 4 NHCO NMe Bu                                                           3-820 4 NHCO NMe HOOCCH.sub.2 --                                              3-821 4 NHCO NMe MeOOCCH.sub.2 --                                             3-822 4 NHCO NMe MeCH(COOH)                                                   3-823 4 NHCO NMe HOOC--(CH.sub.2).sub.2 --                                    3-824 4 NHCO NMe MeCH(COOMe)                                                  3-825 4 NHCO NMe 1-HOOC-iBu                                                   3-826 4 NHCO NMe 1-MeOOC-iBu                                                  3-827 4 NHCO NMe 1-HOOC-iPn                                                   3-828 4 NHCO NMe 1-MeOOC-iPn                                                  3-829 4 NHCO NMe 1-HOOC-2-Me--Bu                                              3-830 4 NHCO NMe 1-MeOOC-2-Me--Bu                                             3-831 4 NHCO NMe CH.sub.2 CH.sub.2 SO.sub.3 H                                 3-832 4 NHCO NMe OH                                                           3-833 4 NHCO NMe MeO                                                          3-834 4 NHCO NMe EtO                                                          3-835 4 NHCO NMe PrO                                                          3-836 4 NHCO NMe iPrO                                                         3-837 4 NHCO NMe BuO                                                          3-838 4 NHCO NMe iBuO                                                         3-839 4 NHCO NMe sBuO                                                         3-840 4 NHCO NMe tBuO                                                         3-841 4 NHCO NMe HxO                                                          3-842 4 NHCO NMe PhO                                                          3-843 4 NHCO NMe BnO                                                          3-844 4 NHCO NMe Z-1                                                          3-845 4 NHCO NMe Z-2                                                          3-846 4 NHCO NMe Z-3                                                          3-847 4 NHCO NMe Z-4                                                          3-848 4 NHCO NMe Z-5                                                          3-849 4 NHCO NMe Z-6                                                          3-850 4 NHCO NMe Z-7                                                          3-851 4 NHCO NMe Z-8                                                          3-852 4 NHCO NMe Z-9                                                          3-853 4 NHCO NMe Z-10                                                         3-854 4 NHCO NMe Z-11                                                         3-855 4 NHCO NMe Z-12                                                         3-856 4 NHCO NMe 3-Py                                                         3-857 4 NHCO NMe 4-Py                                                       3-858 4     NHCO         NHNH   H                                               3-859 4 NHCO NHNH Me                                                          3-860 4 NHCO NHNH Et                                                          3-861 4 NHCO NHNMe Me                                                         3-862 4 NHCO NHNMe Et                                                         3-863 4 NHCO NHNMe Pr                                                       3-864 4     NHCONHNHCO     NH   H                                               3-865 4 NHCONHNHCO NH Ph                                                      3-866 4 NHCONHNHCO NH 2-Me--Ph                                                3-867 4 NHCONHNHCO NH 4-Me--Ph                                                3-868 4 NHCONHNHCO NH 2,4-diMe--Ph                                            3-869 4 NHCONHNHCO NH 3,4-diMe--Ph                                            3-870 4 NHCONHNHCO NH 2-(CF.sub.3)Ph                                          3-871 4 NHCONHNHCO NH 4-(CF.sub.3)Ph                                          3-872 4 NHCONHNHCO NH 2-MeOPh                                                 3-873 4 NHCONHNHCO NH 4-MeOPh                                                 3-874 4 NHCONHNHCO NH 2-EtOPh                                                 3-875 4 NHCONHNHCO NH 4-EtOPh                                                 3-876 4 NHCONHNHCO NH 2-HOPh                                                  3-877 4 NHCONHNHCO NH 4-HOPh                                                  3-878 4 NHCONHNHCO NH 2-(HOOC)Ph                                              3-879 4 NHCONHNHCO NH 4-(HOOC)Ph                                              3-880 4 NHCONHNHCO NH 2-(MeOOC)Ph                                             3-881 4 NHCONHNHCO NH 4-(MeOOC)Ph                                             3-882 4 NHCONHNHCO NH 2-(EtOOC)Ph                                             3-883 4 NHCONHNHCO NH 4-(EtOOC)Ph                                             3-884 4 NHCONHNHCO NH 2-(tBuOOC)Ph                                            3-885 4 NHCONHNHCO NH 4-(tBuOOC)Ph                                            3-886 4 NHCONHNHCO NH 2-Cl--Ph                                                3-887 4 NHCONHNHCO NH 4-Cl--Ph                                                3-888 4 NHCONHNHCO NH 2-Br--Ph                                                3-889 4 NHCONHNHCO NH 4-Br--Ph                                                3-890 4 NHCONHNHCO NH 2-I--Ph                                                 3-891 4 NHCONHNHCO NH 4-I--Ph                                                 3-892 4 NHCONHNHCO NH 2-NO2--Ph                                               3-893 4 NHCONHNHCO NH 4-NO.sub.2 --Ph                                         3-894 4 NHCONHNHCO NH 2-NH.sub.2 --Ph                                         3-895 4 NHCONHNHCO NH 4-NH.sub.2 --Ph                                         3-896 4 NHCONHNHCO NH 2-(HO.sub.3 S)Ph                                        3-897 4 NHCONHNHCO NH 4-(HO.sub.3 S)Ph                                        3-898 4 NHCONHNHCO NH 2-(NH.sub.2 O.sub.2 S)Ph                                3-899 4 NHCONHNHCO NH 4-(NH.sub.2 O.sub.2 S)Ph                                3-900 4 NHCONHNHCO NH 2-CN--Ph                                                3-901 4 NHCONHNHCO NH 4-CN--Ph                                                3-902 4 NHCONHNHCO NH 2-(HOCH.sub.2)Ph                                        3-903 4 NHCONHNHCO NH 4-(HOCH.sub.2)Ph                                        3-904 4 NHCONHNHCO NH Me                                                      3-905 4 NHCONHNHCO NH Et                                                      3-906 4 NHCONHNHCO NH Pr                                                      3-907 4 NHCONHNHCO NH iPr                                                     3-908 4 NHCONHNHCO NH Bu                                                      3-909 4 NHCONHNHCO NH HOOCCH.sub.2 --                                         3-910 4 NHCONHNHCO NH MeOOCCH.sub.2 --                                        3-911 4 NHCONHNHCO NH MeCH(COOH)                                              3-912 4 NHCONHNHCO NH HOOC--(CH.sub.2).sub.2 --                               3-913 4 NHCONHNHCO NH MeCH(COOMe)                                             3-914 4 NHCONHNHCO NH 1-HOOC-iBu                                              3-915 4 NHCONHNHCO NH 1-MeOOC-iBu                                             3-916 4 NHCONHNHCO NH 1-HOOC-iPn                                              3-917 4 NHCONHNHCO NH 1-MeOOC-iPn                                             3-918 4 NHCONHNHCO NH 1-HOOC-2-Me--Bu                                         3-919 4 NHCONHNHCO NH 1-MeOOC-2-Me--Bu                                        3-920 4 NHCONHNHCO NH CH.sub.2 CH.sub.2 SO.sub.3 H                            3-921 4 NHCONHNHCO NH OH                                                      3-922 4 NHCONHNHCO NH MeO                                                     3-923 4 NHCONHNHCO NH EtO                                                     3-924 4 NHCONHNHCO NH PrO                                                     3-925 4 NHCONHNHCO NH iPrO                                                    3-926 4 NHCONHNHCO NH BuO                                                     3-927 4 NHCONHNHCO NH iBuO                                                    3-928 4 NHCONHNHCO NH sBuO                                                    3-929 4 NHCONHNHCO NH tBuO                                                    3-930 4 NHCONHNHCO NH HxO                                                     3-931 4 NHCONHNHCO NH PhO                                                     3-932 4 NHCONHNHCO NH BnO                                                     3-933 4 NHCONHNHCO NH Z-1                                                     3-934 4 NHCONHNHCO NH Z-2                                                     3-935 4 NHCONHNHCO NH Z-3                                                     3-936 4 NHCONHNHCO NH Z-4                                                     3-937 4 NHCONHNHCO NH Z-5                                                     3-938 4 NHCONHNHCO NH Z-6                                                     3-939 4 NHCONHNHCO NH Z-7                                                     3-940 4 NHCONHNHCO NH Z-8                                                     3-941 4 NHCONHNHCO NH Z-9                                                     3-942 4 NHCONHNHCO NH Z-10                                                    3-943 4 NHCONHNHCO NH Z-11                                                    3-944 4 NHCONHNHCO NH Z-12                                                    3-945 4 NHCONHNHCO NH 3-Py                                                    3-946 4 NHCONHNHCO NH 4-Py                                                    3-947 4 NHCONHCO -- H                                                         3-948 4 NHCONHCO -- Ph                                                        3-949 4 NHCONHCO -- 2-Me--Ph                                                  3-950 4 NHCONHCO -- 4-Me--Ph                                                  3-951 4 NHCONHCO -- 2,4-diMe--Ph                                              3-952 4 NHCONHCO -- 3,4-diMe--Ph                                              3-953 4 NHCONHCO -- 2-(CF.sub.3)Ph                                            3-954 4 NHCONHCO -- 4-(CF.sub.3)Ph                                            3-955 4 NHCONHCO -- 2-MeOPh                                                   3-956 4 NHCONHCO -- 4-MeOPh                                                   3-957 4 NHCONHCO -- 2-EtOPh                                                   3-958 4 NHCONHCO -- 4-EtOPh                                                   3-959 4 NHCONHCO -- 2-HOPh                                                    3-960 4 NHCONHCO -- 4-HOPh                                                    3-961 4 NHCONHCO -- 2-(HOOC)Ph                                                3-962 4 NHCONHCO -- 4-(HOOC)Ph                                                3-963 4 NHCONHCO -- 2-(MeOOC)Ph                                               3-964 4 NHCONHCO -- 4-(MeOOC)Ph                                               3-965 4 NHCONHCO -- 2-(EtOOC)Ph                                               3-966 4 NHCONHCO -- 4-(EtOOC)Ph                                               3-967 4 NHCONHCO -- 2-(tBuOOC)Ph                                              3-968 4 NHCONHCO -- 4-(tBuOOC)Ph                                              3-969 4 NHCONHCO -- 2-Cl--Ph                                                  3-970 4 NHCONHCO -- 4-Cl--Ph                                                  4-971 4 NHCONHCO -- 2-Br--Ph                                                  3-972 4 NHCONHCO -- 4-Br--Ph                                                  3-973 4 NHCONHCO -- 2-I--Ph                                                   3-974 4 NHCONHCO -- 4-I--Ph                                                   3-975 4 NHCONHCO -- 2-NO.sub.2 --Ph                                           3-976 4 NHCONHCO -- 4-NO.sub.2 --Ph                                           3-977 4 NHCONHCO -- 2-NH.sub.2 --Ph                                           3-978 4 NHCONHCO -- 4-NH.sub.2 --Ph                                           3-979 4 NHCONHCO -- 2-(HO.sub.3 S)Ph                                          3-980 4 NHCONHCO -- 4-(HO.sub.3 S)Ph                                          3-981 4 NHCONHCO -- 2-(NH.sub.2 O.sub.2 S)Ph                                  3-982 4 NHCONHCO -- 4-(NH.sub.2 O.sub.2 S)Ph                                  3-983 4 NHCONHCO -- 2-CN--Ph                                                  3-984 4 NHCONHCO -- 4-CN--Ph                                                  3-985 4 NHCONHCO -- 2-(HOCH.sub.2)Ph                                          3-986 4 NHCONHCO -- 4-(HOCH.sub.2)Ph                                          3-987 4 NHCONHCO -- Me                                                        3-988 4 NHCONHCO -- Et                                                        3-989 4 NHCONHCO -- Pr                                                        3-990 4 NHCONHCO -- iPr                                                       3-991 4 NHCONHCO -- Bu                                                        3-992 4 NHCONHCO -- HOOCCH.sub.2 --                                           3-993 4 NHCONHCO -- MeOOCCH.sub.2 --                                          3-994 4 NHCONHCO -- MeCH(COOH)                                                3-995 4 NHCONHCO -- HOOC--(CH.sub.2).sub.2 --                                 3-996 4 NHCONHCO -- MeCH(COOMe)                                               3-997 4 NHCONHCO -- 1-HOOC-iBu                                                3-998 4 NHCONHCO -- 1-MeOOC-iBu                                               3-999 4 NHCONHCO -- 1-HOOC-iPn                                                3-1000 4 NHCONHCO -- 1-MeOOC-iPn                                              3-1001 4 NHCONHCO -- 1-HOOC-2-Me--Bu                                          3-1002 4 NHCONHCO -- 1-MeOOC-2-Me--Bu                                         3-1003 4 NHCONHCO -- CH.sub.2 CH.sub.2 SO.sub.3 H                             3-1004 4 NHCONHCO -- MeO                                                      3-1005 4 NHCONHCO -- EtO                                                      3-1006 4 NHCONHCO -- PrO                                                      3-1007 4 NHCONHCO -- iPrO                                                     3-1008 4 NHCONHCO -- BuO                                                      3-1009 4 NHCONHCO -- iBuO                                                     3-1010 4 NHCONHCO -- sBuO                                                     3-1011 4 NHCONHCO -- tBuO                                                     3-1012 4 NHCONHCO -- HxO                                                      3-1013 4 NHCONHCO -- PhO                                                      3-1014 4 NHCONHCO -- BnO                                                      3-1015 4 NHCONHCO -- Z-1                                                      3-1016 4 NHCONHCO -- Z-2                                                      3-1017 4 NHCONHCO -- Z-3                                                      3-1018 4 NHCONHCO -- Z-4                                                      3-1019 4 NHCONHCO -- Z-5                                                      3-1020 4 NHCONHCO -- Z-6                                                      3-1021 4 NHCONHCO -- Z-7                                                      3-1022 4 NHCONHCO -- Z-8                                                      3-1023 4 NHCONHCO -- Z-9                                                      3-1024 4 NHCONHCO -- Z-10                                                     3-1025 4 NHCONHCO -- Z-11                                                     3-1026 4 NHCONHCO -- Z-12                                                     3-1027 4 NHCONHCO -- 3-Py                                                     3-1028 4 NHCONHCO -- 4-Py                                                     3-1029 4 NHCONHSO.sub.2 -- H                                                  3-1030 4 NHCONHSO.sub.2 -- Ph                                                 3-1031 4 NHCONHSO.sub.2 -- 2-Me--Ph                                           3-1032 4 NHCONHSO.sub.2 -- 4-Me--Ph                                           3-1033 4 NHCONHSO.sub.2 -- 2,4-diMe--Ph                                       3-1034 4 NHCONHSO.sub.2 -- 3,4-diMe--Ph                                       3-1035 4 NHCONHSO.sub.2 -- 2-(CF.sub.3)Ph                                     3-1036 4 NHCONHSO.sub.2 -- 4-(CF.sub.3)Ph                                     3-1037 4 NHCONHSO.sub.2 -- 2-MeOPh                                            3-1038 4 NHCONHSO.sub.2 -- 4-MeOPh                                            3-1039 4 NHCONHSO.sub.2 -- 2-EtOPh                                            3-1040 4 NHCONHSO.sub.2 -- 4-EtOPh                                            3-1041 4 NHCONHSO.sub.2 -- 2-HOPh                                             3-1042 4 NHCONHSO.sub.2 -- 4-HOPh                                             3-1043 4 NHCONHSO.sub.2 -- 2-(HOOC)Ph                                         3-1044 4 NHCONHSO.sub.2 -- 4-(HOOC)Ph                                         3-1045 4 NHCONHSO.sub.2 -- 2-(MeOOC)Ph                                        3-1046 4 NHCONHSO.sub.2 -- 4-(MeOOC)Ph                                        3-1047 4 NHCONHSO.sub.2 -- 2-(EtOOC)Ph                                        3-1048 4 NHCONHSO.sub.2 -- 4-(EtOOC)Ph                                        3-1049 4 NHCONHSO.sub.2 -- 2-(tBuOOC)Ph                                       3-1050 4 NHCONHSO.sub.2 -- 4-(tBuOOC)Ph                                       3-1051 4 NHCONHSO.sub.2 -- 2-Cl--Ph                                           3-1052 4 NHCONHSO.sub.2 -- 4-Cl--Ph                                           3-1053 4 NHCONHSO.sub.2 -- 2-Br--Ph                                           3-1054 4 NHCONHSO.sub.2 -- 4-Br--Ph                                           3-1055 4 NHCONHSO.sub.2 -- 2-I--Ph                                            3-1056 4 NHCONHSO.sub.2 -- 4-I--Ph                                            3-1057 4 NHCONSHO.sub.2 -- 2-NO.sub.2 --Ph                                    3-1058 4 NHCONHSO.sub.2 -- 4-NO.sub.2 --Ph                                    3-1059 4 NHCONHSO.sub.2 -- 2-NH.sub.2 --Ph                                    3-1060 4 NHCONHSO.sub.2 -- 4-NH.sub.2 --Ph                                    3-1061 4 NHCONHSO.sub.2 -- 2-(HO.sub.3 S)Ph                                   3-1062 4 NHCONHSO.sub.2 -- 4-(HO.sub.3 S)Ph                                   3-1063 4 NHCONHSO.sub.2 -- 2-(NH.sub.2 O.sub.2 S)Ph                           3-1064 4 NHCONHSO.sub.2 -- 4-(NH.sub.2 O.sub.2 S)Ph                           3-1065 4 NHCONHSO.sub.2 -- 2-CN--Ph                                           3-1066 4 NHCONHSO.sub.2 -- 4-CN--Ph                                           3-1067 4 NHCONHSO.sub.2 -- 2-(HOCH.sub.2)Ph                                   3-1068 4 NHCONHSO.sub.2 -- 4-(HOCH.sub.2)Ph                                   3-1069 4 NHCONHSO.sub.2 -- Me                                                 3-1070 4 NHCONHSO.sub.2 -- Et                                                 3-1071 4 NHCONHSO.sub.2 -- Pr                                                 3-1072 4 NHCONHSO.sub.2 -- iPr                                                3-1073 4 NHCONHSO.sub.2 -- Bu                                                 3-1074 4 NHCONHSO.sub.2 -- HOOCCH.sub.2 --                                    3-1075 4 NHCONHSO.sub.2 -- MeOOCCH.sub.2 --                                   3-1076 4 NHCONHSO.sub.2 -- MeCH(COOH)                                         3-1077 4 NHCONHSO.sub.2 -- HOOC--(CH.sub.2).sub.2 --                          3-1078 4 NHCONHSO.sub.2 -- MeCH(COOMe)                                        3-1079 4 NHCONHSO.sub.2 -- 1-HOOC-iBu                                         3-1080 4 NHCONHSO.sub.2 -- 1-MeOOC-iBu                                        3-1081 4 NHCONHSO.sub.2 -- 1-HOOC-iPn                                         3-1082 4 NHCONHSO.sub.2 -- 1-MeOOC-iPn                                        3-1083 4 NHCONHSO.sub.2 -- 1-HOOC-2-Me--Bu                                    3-1084 4 NHCONHSO.sub.2 -- 1-MeOOC-2-Me--Bu                                   3-1085 4 NHCONHSO.sub.2 -- CH.sub.2 CH.sub.2 SO.sub.3 H                       3-1086 4 NHCONHSO.sub.2 -- OH                                                 3-1087 4 NHCONHSO.sub.2 -- MeO                                                3-1088 4 NHCONHSO.sub.2 -- EtO                                                3-1089 4 NHCONHSO.sub.2 -- PrO                                                3-1090 4 NHCONHSO.sub.2 -- iPrO                                               3-1091 4 NHCONHSO.sub.2 -- BuO                                                3-1092 4 NHCONHSO.sub.2 -- iBuO                                               3-1093 4 NHCONHSO.sub.2 -- sBuO                                               3-1094 4 NHCONHSO.sub.2 -- tBuO                                               3-1095 4 NHCONHSO.sub.2 -- HxO                                                3-1096 4 NHCONHSO.sub.2 -- PhO                                                3-1097 4 NHCONHSO.sub.2 -- BnO                                                3-1098 4 NHCONHSO.sub.2 -- Z-1                                                3-1099 4 NHCONHSO.sub.2 -- Z-2                                                3-1100 4 NHCONHSO.sub.2 -- Z-3                                                3-1101 4 NHCONHSO.sub.2 -- Z-4                                                3-1102 4 NHCONHSO.sub.2 -- Z-5                                                3-1103 4 NHCONHSO.sub.2 -- Z-6                                                3-1104 4 NHCONHSO.sub.2 -- Z-7                                                3-1105 4 NHCONHSO.sub.2 -- Z-8                                                3-1106 4 NHCONHSO.sub.2 -- Z-9                                                3-1107 4 NHCONHSO.sub.2 -- Z-10                                               3-1108 4 NHCONHSO.sub.2 -- Z-11                                               3-1109 4 NHCONHSO.sub.2 -- Z-12                                               3-1110 4 NHCONHSO.sub.2 -- 3-Py                                               3-1111 4 NHCONHSO.sub.2 -- 4-Py                                               3-1112 4 NHCONHSO.sub.2 NH H                                                  3-1113 4 NHCONHSO.sub.2 NH Me                                                 3-1114 4 NHCONHSO.sub.2 NH Et                                                 3-1115 4 NHCONHSO.sub.2 NH Pr                                                 3-1116 4 NHCONHSO.sub.2 NH iPr                                                3-1117 4 NHCONHSO.sub.2 NH Bu                                                 3-1118 4 NHCONHSO.sub.2 NMe Me                                                3-1119 4 NHCONHSO.sub.2 NMe Et                                                3-1120 4 NHCONHSO.sub.2 NMe Pr                                                3-1121 4 NHCONHSO.sub.2 NMe iPr                                               3-1122 4 NHCONHSO.sub.2 NMe Bu                                                3-1123 4 -- NH H                                                              3-1124 4 -- NH Me                                                             3-1125 4 -- NH Et                                                             3-1126 4 -- NH Pr                                                             3-1127 4 -- NH iPr                                                            3-1128 4 -- NH Bu                                                           3-1129                                                                              4     CO             Pyr                                                  3-1130 4 CO Pipri                                                             3-1131 4 CO Pipra                                                             3-1132 4 CO Mor                                                               3-1133 4 CO Thmor                                                             3-1134 4 CO NHPyr                                                             3-1135 4 CO NHPipri                                                           3-1136 4 CO NHPipra                                                           3-1137 4 CO NHMor                                                             3-1138 4 CO NHThmor                                                           3-1139 4 NHCO Pyr                                                             3-1140 4 NHCO Pipri                                                           3-1141 4 NHCO Pipra                                                           3-1142 4 NHCO Mor                                                             3-1143 4 NHCO Thmor                                                           3-1144 4 NHCO NHPyr                                                           3-1145 4 NHCO NHPipri                                                         3-1146 4 NHCO NHPipra                                                         3-1147 4 NHCO NHMor                                                           3-1148 4 NHCO NHThmor                                                         3-1149 4 CONHCO Pyr                                                           3-1150 4 CONHCO Pipri                                                         3-1151 4 CONHCO Pipra                                                         3-1152 4 CONHCO Mor                                                           3-1153 4 CONHCO Thmor                                                         3-1154 4 CONHCO NHPyr                                                         3-1155 4 CONHCO NHPipri                                                       3-1156 4 CONHCO NHPipra                                                       3-1157 4 CONHCO NHMor                                                         3-1158 4 CONHCO NHThmor                                                       3-1159 4 CONHSO.sub.2 Pyr                                                     3-1160 4 CONHSO.sub.2 Pipri                                                   3-1161 4 CONHSO.sub.2 Pipra                                                   3-1162 4 CONHSO.sub.2 Mor                                                     3-1163 4 CONHSO.sub.2 Thmor                                                   3-1164 4 CONHSO.sub.2 NHPyr                                                   3-1165 4 CONHSO.sub.2 NHPipri                                                 3-1166 4 CONHSO.sub.2 NHPipra                                                 3-1167 4 CONHSO.sub.2 NHMor                                                   3-1168 4 CONHSO.sub.2 NHThmor                                               3-1169                                                                              4     NHSO.sub.2     NH   Z-4                                             3-1170 4 NHSO.sub.2 -- Me                                                     3-1171 4 NHSO.sub.2 -- Et                                                     3-1172 4 NHSO.sub.2 -- Pr                                                     3-1173 4 NHSO.sub.2 -- CH.sub.2--Cl                                           3-1174 4 NHSO.sub.2 -- Ph                                                     3-1175 4 NHSO.sub.2 -- 4-Me--Ph                                               3-1176 4 CO NMe Ph                                                            3-1177 4 CO NMe 2-Me--Ph                                                      3-1178 4 CO NMe 4-Me--Ph                                                      3-1179 4 CO NMe 2,4-diMe--Ph                                                  3-1180 4 CO NMe 3,4-diMe--Ph                                                  3-1181 4 CO NMe 2-(CF.sub.3)Ph                                                3-1182 4 CO NMe 4-(CF.sub.3)Ph                                                3-1183 4 CO NMe 2-MeOPh                                                       3-1184 4 CO NMe 4-MeOPh                                                       3-1185 4 CO NMe 2-EtOPh                                                       3-1186 4 CO NMe 4-EtOPh                                                       3-1187 4 CO NMe 2-HOPh                                                        3-1188 4 CO NMe 4-HOPh                                                        3-1189 4 CO NMe 2-(HOOC)Ph                                                    3-1190 4 CO NMe 4-(HOOC)Ph                                                    3-1191 4 CO NMe 2-(MeOOC)Ph                                                   3-1192 4 CO NMe 4-(MeOOC)Ph                                                   3-1193 4 CO NMe 2-(EtOOC)Ph                                                   3-1194 4 CO NMe 4-(EtOOC)Ph                                                   3-1195 4 CO NMe 2-(tBuOOC)Ph                                                  3-1196 4 CO NMe 4-(tBuOOC)Ph                                                  3-1197 4 CO NMe 2-Cl--Ph                                                      3-1198 4 CO NMe 4-Cl--Ph                                                      3-1199 4 CO NMe 2-Br--Ph                                                      3-1200 4 CO NMe 4-Br--Ph                                                      3-1201 4 CO NMe 2-I--Ph                                                       3-1202 4 CO NMe 4-I--Ph                                                       3-1203 4 CO NMe 2-NO.sub.2 --Ph                                               3-1204 4 CO NMe 4-NO.sub.2 --Ph                                               3-1205 4 CO NMe 2-NH.sub.2 --Ph                                               3-1206 4 CO NMe 4-NH.sub.2 --Ph                                               3-1207 4 CO NMe 2-(HO.sub.3 S)Ph                                              3-1208 4 CO NMe 4-(HO.sub.3 S)Ph                                              3-1209 4 CO NMe 2-(NH.sub.2 O.sub.2 S)Ph                                      3-1210 4 CO NMe 4-(NH.sub.2 O.sub.2 S)Ph                                      3-1211 4 CO NMe 2-CN--Ph                                                      3-1212 4 CO NMe 4-CN--Ph                                                      3-1213 4 CO NMe 2-(HOCH.sub.2)Ph                                              3-1214 4 CO NMe 4-(HOCH.sub.2)Ph                                              3-1215 4 CO NMe Me                                                            3-1216 4 CO NMe Et                                                            3-1217 4 CO NMe Pr                                                            3-1218 4 CO NMe iPr                                                           3-1219 4 CO NMe Bu                                                            3-1220 4 CO NMe HOOCCH.sub.2 --                                               3-1221 4 CO NMe MeOOCCH.sub.2 --                                              3-1222 4 CO NMe MeCH(COOH)                                                    3-1223 4 CO NMe HOOC--(CH.sub.2).sub.2 --                                     3-1224 4 CO NMe MeCH(COOMe)                                                   3-1225 4 CO NMe 1-HOOC-iBu                                                    3-1226 4 CO NMe 1-MeOOC-iBu                                                   3-1227 4 CO NMe 1-HOOC-iPn                                                    3-1228 4 CO NMe 1-MeOOC-iPn                                                   3-1229 4 CO NMe 1-HOOC-2-Me--Bu                                               3-1230 4 CO NMe 1-MeOOC-2-Me--Bu                                              3-1231 4 CO NMe CH.sub.2 CH.sub.2 SO.sub.3 H                                  3-1232 4 CO NMe OH                                                            3-1233 4 CO NMe MeO                                                           3-1234 4 CO NMe EtO                                                           3-1235 4 CO NMe PrO                                                           3-1236 4 CO NMe iPrO                                                          3-1237 4 CO NMe BuO                                                           3-1238 4 CO NMe iBuO                                                          3-1239 4 CO NMe sBuO                                                          3-1240 4 CO NMe tBuO                                                          3-1241 4 CO NMe HxO                                                           3-1242 4 CO NMe PhO                                                           3-1243 4 CO NMe BnO                                                           3-1244 4 CO NMe Z-1                                                           3-1245 4 CO NMe Z-2                                                           3-1246 4 CO NMe Z-3                                                           3-1247 4 CO NMe Z-4                                                           3-1248 4 CO NMe Z-5                                                           3-1249 4 CO NMe Z-6                                                           3-1250 4 CO NMe Z-7                                                           3-1251 4 CO NMe Z-8                                                           3-1252 4 CO NMe Z-9                                                           3-1253 4 CO NMe Z-10                                                          3-1254 4 CO NMe Z-11                                                          3-1255 4 CO NMe Z-12                                                          3-1256 4 CO NMe 3-Py                                                          3-1257 4 CO NMe 4-Py                                                        3-1258                                                                              4     CO             Thiad                                                3-1259 4 CO NHThiad                                                           3-1260 4 NHCO Thiad                                                           3-1261 4 NHCO NHThiad                                                         3-1262 4 CONHCO Thiad                                                         3-1263 4 CONHCO NHThiad                                                       3-1264 4 CONHSO.sub.2 Thiad                                                   3-1265 4 CONHSO.sub.2 NHThiad                                               3-1266                                                                              4     NHCS           NH   H                                               3-1267 4 NHCS NH Me                                                           3-1268 4 NHCS NH Et                                                           3-1269 4 NHCS NH Ph                                                           3-1270 4 NHCS NH HOOCCH.sub.2 --                                              3-1271 4 NHCS NH MeOOCCH.sub.2 --                                             3-1272 4 NHCS NH MeCH(COOH)                                                   3-1273 4 NHCS NH HOOC--(CH.sub.2).sub.2 --                                    3-1274 4 NHCS NH MeCH(COOMe)                                                  3-1275 4 CO NH HOOC--(CH.sub.2).sub.3 --                                      3-1276 4 NHCO NH HOOC--(CH.sub.2).sub.3 --                                    3-1277 4 NHCO -- HOOC--(CH.sub.2).sub.3 --                                    3-1278 4 NHCS NH HOOC--(CH.sub.2).sub.3 --                                    3-1279 4 CO NH MeSO.sub.2 NHCOCH(Me)                                          3-1280 4 NHCO NH MeSO.sub.2 NHCOCH(Me)                                        3-1281 4 NHCO -- MeSO.sub.2 NHCOCH(Me)                                        3-1282 4 NHCS NH MeSO.sub.2 NHCOCH(Me)                                        3-1283 4 -- NH HOOCCH.sub.2 --                                                3-1284 4 -- NH MeOOCCH.sub.2 --                                               3-1285 4 -- NH MeCH(COOH)                                                     3-1286 4 -- NH HOOC--(CH.sub.2).sub.2 --                                      3-1287 4 -- NH MeCH(COOMe)                                                    3-1288 4 -- NH HOOC--(CH.sub.2).sub.3 --                                      3-1289 4 NHCOCO -- OH                                                         3-1290 4 NHCOCO -- MeO                                                        3-1291 4 NHCOCO -- EtO                                                        3-1292 4 NHCOCO -- PrO                                                        3-1293 4 NHCOCO -- iPrO                                                       3-1294 4 NHCOCO -- BuO                                                        3-1295 4 NHCOCO -- iBuO                                                       3-1296 4 NHCOCO -- sBuO                                                       3-1297 4 NHCOCO -- tBuO                                                       3-1298 4 NHCOCO -- HxO                                                        3-1299 4 NHCOCO -- PhO                                                        3-1300 4 NHCOCO -- BnO                                                        3-1301 5 CO NH H                                                              3-1302 5 CO NH Ph                                                             3-1303 5 CO NH 2-Me--Ph                                                       3-1304 5 CO NH 4-Me--Ph                                                       3-1305 5 CO NH 2,4-diMe--Ph                                                   3-1306 5 CO NH 3,4-diMe--Ph                                                   3-1307 5 CO NH 2-(CF.sub.3)Ph                                                 3-1308 5 CO NH 4-(CF.sub.3)Ph                                                 3-1309 5 CO NH 2-MeOPh                                                        3-1310 5 CO NH 4-MeOPh                                                        3-1311 5 CO NH 2-EtOPh                                                        3-1312 5 CO NH 4-EtOPh                                                        3-1313 5 CO NH 2-HOPh                                                         3-1314 5 CO NH 4-HOPh                                                         3-1315 5 CO NH 2-(HOOC)Ph                                                     3-1316 5 CO NH 4-(HOOC)Ph                                                     3-1317 5 CO NH 2-(MeOOC)Ph                                                    3-1318 5 CO NH 4-(MeOOC)Ph                                                    3-1319 5 CO NH 2-(EtOOC)Ph                                                    3-1320 5 CO NH 4-(EtOOC)Ph                                                    3-1321 5 CO NH 2-(tBuOOC)Ph                                                   3-1322 5 CO NH 4-(tBuOOC)Ph                                                   3-1323 5 CO NH 2-Cl--Ph                                                       3-1324 5 CO NH 4-Cl--Ph                                                       3-1325 5 CO NH 2-Br--Ph                                                       3-1326 5 CO NH 4-Br--Ph                                                       3-1327 5 CO NH 2-I--Ph                                                        3-1328 5 CO NH 4-I--Ph                                                        3-1329 5 CO NH 2-NO.sub.2 --Ph                                                3-1330 5 CO NH 4-NO.sub.2 --Ph                                                3-1331 5 CO NH 2-NH.sub.2 --Ph                                                3-1332 5 CO NH 4-NH.sub.2 --Ph                                                3-1333 5 CO NH 2-(HO.sub.3 S)Ph                                               3-1334 5 CO NH 4-(HO.sub.3 S)Ph                                               3-1335 5 CO NH 2-(NH.sub.2 O.sub.2 S)Ph                                       3-1336 5 CO NH 4-(NH.sub.2 O.sub.2 S)Ph                                       3-1337 5 CO NH 2-CN--Ph                                                       3-1338 5 CO NH 4-CN--Ph                                                       3-1339 5 CO NH 2-(HOCH.sub.2)Ph                                               3-1340 5 CO NH 4-(HOCH.sub.2)Ph                                               3-1341 5 CO NH Me                                                             3-1342 5 CO NH Et                                                             3-1343 5 CO NH Pr                                                             3-1344 5 CO NH iPr                                                            3-1345 5 CO NH Bu                                                             3-1346 5 CO NH HOOCCH.sub.2 --                                                3-1347 5 CO NH MeOOCCH.sub.2 --                                               3-1348 5 CO NH MeCH(COOH)                                                     3-1349 5 CO NH HOOC--(CH.sub.2).sub.2 --                                      3-1350 5 CO  NH MeCH(COOMe)                                                   3-1351 5 CO NH 1-HOOC-iBu                                                     3-1352 5 CO NH 1-MeOOC-iBu                                                    3-1353 5 CO NH 1-HOOC-iPn                                                     3-1354 5 CO NH 1-MeOOC-iPn                                                    3-1355 5 CO NH 1-HOOC-2-Me--Bu                                                3-1356 5 CO NH 1-MeOOC-2-Me--Bu                                               3-1357 5 CO NH CH.sub.2 CH.sub.2 SO.sub.3 H                                   3-1358 5 CO NH OH                                                             3-1359 5 CO NH MeO                                                            3-1360 5 CO NH EtO                                                            3-1361 5 CO NH PrO                                                            3-1362 5 CO NH iPrO                                                           3-1363 5 CO NH BuO                                                            3-1364 5 CO NH iBuO                                                           3-1365 5 CO NH sBuO                                                           3-1366 5 CO NH tBuO                                                           3-1367 5 CO NH HxO                                                            3-1368 5 CO NH PhO                                                            3-1369 5 CO NH BnO                                                            3-1370 5 CO NH Z-1                                                            3-1371 5 CO NH Z-2                                                            3-1372 5 CO NH Z-3                                                            3-1373 5 CO NH Z-4                                                            3-1375 5 CO NH Z-6                                                            3-1376 5 CO NH Z-7                                                            3-1377 5 CO NH Z-8                                                            3-1378 5 CO NH Z-9                                                            3-1379 5 CO NH Z-10                                                           3-1380 5 CO NH Z-11                                                           3-1381 5 CO NH Z-12                                                           3-1382 5 CO NH 3-Py                                                           3-1383 5 CO NH 4-Py                                                           3-1384 5 CO N(Ac) H                                                           3-1385 5 CO N(Ac) Ph                                                          3-1386 5 CO N(Ac) 2-Me--Ph                                                    3-1387 5 CO N(Ac) 4-Me--Ph                                                    3-1388 5 CO N(Ac) 2,4-diMe--Ph                                                3-1389 5 CO N(Ac) 3,4-diMe--Ph                                                3-1390 5 CO N(Ac) 2-(CF.sub.3)Ph                                              3-1391 5 CO N(Ac) 4-(CF.sub.3)Ph                                              3-1392 5 CO N(Ac) 2-MeOPh                                                     3-1393 5 CO N(Ac) 4-MeOPh                                                     3-1394 5 CO N(Ac) 2-EtOPh                                                     3-1395 5 CO N(Ac) 4-EtOPh                                                     3-1396 5 CO N(Ac) 2-HOPh                                                      3-1397 5 CO N(Ac) 4-HOPh                                                      3-1398 5 CO N(Ac) 2-(HOOC)Ph                                                  3-1399 5 CO N(Ac) 4-(HOOC)Ph                                                  3-1400 5 CO N(Ac) 2-(MeOOC)Ph                                                 3-1401 5 CO N(Ac) 4-(MeOOC)Ph                                                 3-1402 5 CO N(Ac) 2-(EtOOC)Ph                                                 3-1403 5 CO N(Ac) 4-(EtOOC)Ph                                                 3-1404 5 CO N(Ac) 2-(tBuOOC)Ph                                                3-1405 5 CO N(Ac) 4-(tBuOOC)Ph                                                3-1406 5 CO N(Ac) 2-Cl--Ph                                                    3-1407 5 CO N(Ac) 4-Cl--Ph                                                    3-1408 5 CO N(Ac) 2-Br--Ph                                                    3-1409 5 CO N(Ac) 4-Br--Ph                                                    3-1410 5 CO N(Ac) 2-I--Ph                                                     3-1411 5 CO N(Ac) 4-I--Ph                                                     3-1412 5 CO N(Ac) 2-NO.sub.2 --Ph                                             3-1413 5 CO N(Ac) 4-NO.sub.2 --Ph                                             3-1414 5 CO N(Ac) 2-NH.sub.2 --Ph                                             3-1415 5 CO N(Ac) 4-NH.sub.2 --Ph                                             3-1416 5 CO N(Ac) 2-(HO.sub.3 S)Ph                                            3-1417 5 CO N(Ac) 4-(HO.sub.3 S)Ph                                            3-1419 5 CO N(Ac) 2-(NH.sub.2 O.sub.2 S)Ph                                    3-1420 5 CO N(Ac) 2-CN--Ph                                                    3-1421 5 CO N(Ac) 4-CN--Ph                                                    3-1422 5 CO N(Ac) 2-(HOCH.sub.2)Ph                                            3-1423 5 CO N(Ac) 4-(HOCH.sub.2)Ph                                            3-1424 5 CO N(Ac) Me                                                          3-1425 5 CO N(Ac) Et                                                          3-1426 5 CO N(Ac) Pr                                                          3-1427 5 CO N(Ac) iPr                                                         3-1428 5 CO N(Ac) Bu                                                          3-1429 5 CO N(Ac) HOOCCH.sub.2 --                                             3-1430 5 CO N(Ac) MeOOCCH.sub.2 --                                            3-1431 5 CO N(Ac) MeCH(COOH)                                                  3-1432 5 CO N(Ac) HOOC--(CH.sub.2).sub.2 --                                   3-1433 5 CO N(Ac) MeCH(COOMe)                                                 3-1434 5 CO N(Ac) 1-HOOC-iBu                                                  3-1435 5 CO N(Ac) 1-MeOOC-iBu                                                 3-1436 5 CO N(Ac) 1-HOOC-iPn                                                  3-1437 5 CO N(Ac) 1-MeOOC-iPn                                                 3-1438 5 CO N(Ac) 1-HOOC-2-Me--Bu                                             3-1439 5 CO N(Ac) 1-MeOOC-2-Me--Bu                                            3-1440 5 CO N(Ac) CH.sub.2 CH.sub.2 SO.sub.3 H                                3-1441 5 CO N(Ac) OH                                                          3-1442 5 CO N(Ac) MeO                                                         3-1443 5 CO N(Ac) EtO                                                         3-1444 5 CO N(Ac) PrO                                                         3-1445 5 CO N(Ac) iPrO                                                        3-1446 5 CO N(Ac) BuO                                                         3-1447 5 CO N(Ac) iBuO                                                        3-1448 5 CO N(Ac) sBuO                                                        3-1449 5 CO N(Ac) tBuO                                                        3-1450 5 CO N(Ac) HxO                                                         3-1451 5 CO N(Ac) PhO                                                         3-1452 5 CO N(Ac) BnO                                                         3-1453 5 CO N(Ac) Z-1                                                         3-1454 5 CO N(Ac) Z-2                                                         3-1455 5 CO N(Ac) Z-3                                                         3-1456 5 CO N(Ac) Z-4                                                         3-1457 5 CO N(Ac) Z-5                                                         3-1458 5 CO N(Ac) Z-6                                                         3-1459 5 CO N(Ac) Z-7                                                         3-1460 5 CO N(Ac) Z-8                                                         3-1461 5 CO N(Ac) Z-9                                                         3-1462 5 CO N(Ac) Z-10                                                        3-1463 5 CO N(Ac) Z-11                                                        3-1464 5 CO N(Ac) Z-12                                                        3-1465 5 CO N(Ac) 3-Py                                                        3-1466 5 CO N(Ac) 4-Py                                                        3-1467 5 COO -- H                                                             3-1468 5 COO -- Ph                                                            3-1469 5 COO -- 2-Me--Ph                                                      3-1470 5 COO -- 4-Me--Ph                                                      3-1471 5 COO -- 2,4-diMe--Ph                                                  3-1472 5 COO -- 3,4-diMe--Ph                                                  3-1473 5 COO -- 2-(CF.sub.3)Ph                                                3-1474 5 COO -- 4-(CF.sub.3)Ph                                                3-1475 5 COO -- 2-MeOPh                                                       3-1476 5 COO -- 4-MeOPh                                                       3-1477 5 COO -- 2-EtOPh                                                       3-1478 5 COO -- 4-EtOPh                                                       3-1479 5 COO -- 2-HOPh                                                        3-1480 5 COO -- 4-HOPh                                                        3-1481 5 COO -- 2-(HOOC)Ph                                                    3-1482 5 COO -- 4-(HOOC)Ph                                                    3-1483 5 COO -- 2-(MeOOC)Ph                                                   3-1484 5 COO -- 4-(MeOOC)Ph                                                   3-1485 5 COO -- 2-(EtOOC)Ph                                                   3-1486 5 COO -- 4-(EtOOC)Ph                                                   3-1487 5 COO -- 2-(tBuOOC)Ph                                                  3-1488 5 COO -- 4-(tBuOOC)Ph                                                  3-1489 5 COO -- 2-Cl--Ph                                                      3-1490 5 COO -- 4-Cl--Ph                                                      3-1491 5 COO -- 2-Br--Ph                                                      3-1492 5 COO -- 4-Br--Ph                                                      3-1493 5 COO -- 2-I--Ph                                                       3-1494 5 COO -- 4-I--Ph                                                       3-1495 5 COO -- 2-NO.sub.2 --Ph                                               3-1496 5 COO -- 4-NO.sub.2 --Ph                                               3-1497 5 COO -- 2-NH.sub.2 --Ph                                               3-1498 5 COO -- 4-NH.sub.2 --Ph                                               3-1499 5 COO -- 2-(HO.sub.3 S)Ph                                              3-1500 5 COO -- 4-(HO.sub.3 S)Ph                                              3-1501 5 COO -- 2-(NH.sub.2 O.sub.2 S)Ph                                      3-1502 5 COO -- 4-(NH.sub.2 O.sub.2 S)Ph                                      3-1503 5 COO -- 2-CN--Ph                                                      3-1504 5 COO -- 4-CN--Ph                                                      3-1505 5 COO -- 2-(HOCH.sub.2)Ph                                              3-1506 5 COO -- 4-(HOCH.sub.2)Ph                                              3-1507 5 COO -- Me                                                            3-1508 5 COO -- Et                                                            3-1509 5 COO -- Pr                                                            3-1510 5 COO -- iPr                                                           3-1511 5 COO -- Bu                                                            3-1512 5 COO -- HOOCCH.sub.2 --                                               3-1513 5 COO -- HOOC--(CH.sub.2).sub.2 --                                     3-1514 5 COO -- MeCH(COOMe)                                                   3-1515 5 COO -- 1-HOOC-iBu                                                    3-1516 5 COO -- 1-HOOC-iPn                                                    3-1517 5 COO -- Z-1                                                           3-1518 5 COO -- Z-2                                                           3-1519 5 COO -- Z-3                                                           3-1520 5 COO -- Z-4                                                           3-1521 5 COO -- Z-5                                                           3-1522 5 COO -- Z-6                                                           3-1523 5 COO -- Z-7                                                           3-1524 5 COO -- Z-8                                                           3-1525 5 COO -- Z-9                                                           3-1526 5 COO -- Z-10                                                          3-1527 5 COO -- Z-11                                                          3-1528 5 COO -- Z-12                                                          3-1529 5 COO -- 3-Py                                                          3-1530 5 COO -- 4-Py                                                          3-1531 5 CONHCO -- H                                                          3-1532 5 CONHCO -- Ph                                                         3-1533 5 CONHCO -- 2-Me--Ph                                                   3-1534 5 CONHCO -- 4-Me--Ph                                                   3-1535 5 CONHCO -- 2,4-diMe--Ph                                               3-1536 5 CONHCO -- 3,4-diMe--Ph                                               3-1537 5 CONHCO -- 2-(CF.sub.3)Ph                                             3-1538 5 CONHCO -- 4-(CF.sub.3)Ph                                             3-1539 5 CONHCO -- 2-MeOPh                                                    3-1540 5 CONHCO -- 4-MeOPh                                                    3-1541 5 CONHCO -- 2-EtOPh                                                    3-1542 5 CONHCO -- 4-EtOPh                                                    3-1543 5 CONHCO -- 2-HOPh                                                     3-1544 5 CONHCO -- 4-HOPh                                                     3-1545 5 CONHCO -- 2-(HOOC)Ph                                                 3-1546 5 CONHCO -- 4-(HOOC)Ph                                                 3-1547 5 CONHCO -- 2-(MeOOC)Ph                                                3-1548 5 CONHCO -- 4-(MeOOC)Ph                                                3-1549 5 CONHCO -- 2-(EtOOC)Ph                                                3-1550 5 CONHCO -- 4-(EtOOC)Ph                                                3-1551 5 CONHCO -- 2-(tBuOOC)Ph                                               3-1552 5 CONHCO -- 4-(tBuOOC)Ph                                               3-1553 5 CONHCO -- 2-Cl--Ph                                                   3-1554 5 CONHCO -- 4-Cl--Ph                                                   3-1555 5 CONHCO -- 2-Br--Ph                                                   3-1556 5 CONHCO -- 4-Br--Ph                                                   3-1557 5 CONHCO -- 2-I--Ph                                                    3-1558 5 CONHCO -- 4-I--Ph                                                    3-1559 5 CONHCO -- 2-NO.sub.2 --Ph                                            3-1560 5 CONHCO -- 4-NO.sub.2 --Ph                                            3-1561 5 CONHCO -- 2-NH.sub.2 --Ph                                            3-1562 5 CONHCO -- 4-NH.sub.2 --Ph                                            3-1563 5 CONHCO -- 2-(HO.sub.3 S)Ph                                           3-1564 5 CONHCO -- 4-(HO.sub.3 S)Ph                                           3-1565 5 CONHCO -- 2-(NH.sub.2 O.sub.2 S)Ph                                   3-1566 5 CONHCO -- 4-(NH.sub.2 O.sub.2 S)Ph                                   3-1567 5 CONHCO -- 2-CN--Ph                                                   3-1568 5 CONHCO -- 4-CN--Ph                                                   3-1569 5 CONHCO -- 2-(HOCH.sub.2)Ph                                           3-1570 5 CONHCO -- 4-(HOCH.sub.2)Ph                                           3-1571 5 CONHCO -- Me                                                         3-1572 5 CONHCO -- Et                                                         3-1573 5 CONHCO -- Pr                                                         3-1574 5 CONCHO -- iPr                                                        3-1575 5 CONHCO -- Bu                                                         3-1576 5 CONHCO -- HOOCCH.sub.2 --                                            3-1577 5 CONHCO -- MeOOCCH.sub.2 --                                           3-1578 5 CONHCO -- MeCH(COOH)                                                 3-1579 5 CONHCO -- HOOC--(CH.sub.2).sub.2 --                                  3-1580 5 CONHCO -- MeCH(COOMe)                                                3-1581 5 CONHCO -- 1-HOOC-iBu                                                 3-1582 5 CONHCO -- 1-MeOOC-iBu                                                3-1583 5 CONHCO -- 1-HOOC-iPn                                                 3-1584 5 CONHCO -- 1-MeOOC-iPn                                                3-1585 5 CONHCO -- 1-HOOC-2-Me--Bu                                            3-1586 5 CONHCO -- 1-MeOOC-2-Me--Bu                                           3-1587 5 CONHCO -- CH.sub.2 CH.sub.2 SO.sub.3 H                               3-1588 5 CONHCO -- Z-1                                                        3-1589 5 CONHCO -- Z-2                                                        3-1590 5 CONHCO -- Z-3                                                        3-1591 5 CONHCO -- Z-4                                                        3-1592 5 CONHCO -- Z-5                                                        3-1593 5 CONHCO -- Z-6                                                        3-1594 5 CONHCO -- Z-7                                                        3-1595 5 CONHCO -- Z-8                                                        3-1596 5 CONHCO -- Z-9                                                        3-1597 5 CONHCO -- Z-10                                                       3-1598 5 CONHCO -- Z-11                                                       3-1599 5 CONHCO -- Z-12                                                       3-1600 5 CONHCO -- 3-Py                                                       3-1601 5 CONHCO -- 4-Py                                                       3-1602 5 CON(Ac)CO -- H                                                       3-1603 5 CON(Ac)CO -- Ph                                                      3-1604 5 CON(Ac)CO -- 2-Me--Ph                                                3-1605 5 CON(Ac)CO -- 4-Me--Ph                                                3-1606 5 CON(Ac)CO -- 2,4-diMe--Ph                                            3-1607 5 CON(Ac)CO -- 3,4-diMe--Ph                                            3-1608 5 CON(Ac)CO -- 2-(CF.sub.3)Ph                                          3-1609 5 CON(Ac)CO -- 4-(CF.sub.3)Ph                                          3-1610 5 CON(Ac)CO -- 2-MeOPh                                                 3-1611 5 CON(Ac)CO -- 4-EtOPh                                                 3-1612 5 CON(Ac)CO -- 2-EtOPh                                                 3-1613 5 CON(Ac)CO -- 4-EtOPh                                                 3-1614 5 CON(Ac)CO -- 2-HOPh                                                  3-1615 5 CON(Ac)CO -- 4-HOPh                                                  3-1616 5 CON(Ac)CO -- 2-(HOOC)Ph                                              3-1617 5 CON(Ac)CO -- 4-(HOOC)Ph                                              3-1618 5 CON(Ac)CO -- 2-(MeOOC)Ph                                             3-1619 5 CON(Ac)CO -- 4-(MeOOC)Ph                                             3-1620 5 CON(Ac)CO -- 2-(EtOOC)Ph                                             3-1621 5 CON(Ac)CO -- 4-(EtOOC)Ph                                             3-1622 5 CON(Ac)CO -- 2-(tBuOOC)Ph                                            3-1623 5 CON(Ac)CO -- 4-(tBuOOC)Ph                                            3-1624 5 CON(Ac)CO -- 2-Cl--Ph                                                3-1625 5 CON(Ac)CO -- 4-Cl--Ph                                                3-1626 5 CON(Ac)CO -- 2-Br--Ph                                                3-1627 5 CON(Ac)CO -- 4-Br--Ph                                                3-1628 5 CON(Ac)CO -- 2-I--Ph                                                 3-1629 5 CON(Ac)CO -- 4-I--Ph                                                 3-1630 5 CON(Ac)CO -- 2-NO.sub.2 --Ph                                         3-1631 5 CON(Ac)CO -- 4-NO.sub.2 --Ph                                         3-1632 5 CON(Ac)CO -- 2-NH.sub.2 --Ph                                         3-1633 5 CON(Ac)CO -- 4-NH.sub.2 --Ph                                         3-1634 5 CON(Ac)CO -- 2-(HO.sub.3 S)Ph                                        3-1635 5 CON(Ac)CO -- 4-(HO.sub.3 S)Ph                                        3-1636 5 CON(Ac)CO -- 2-(NH.sub.2 O.sub.2 S)Ph                                3-1637 5 CON(Ac)CO -- 4-(NH.sub.2 O.sub.2 S)Ph                                3-1638 5 CON(Ac)CO -- 2-CN--Ph                                                3-1639 5 CON(Ac)CO -- 4-CN--Ph                                                3-1640 5 CON(Ac)CO -- 2-(HOCH.sub.2)Ph                                        3-1641 5 CON(Ac)CO -- 4-(HOCH.sub.2)Ph                                        3-1642 5 CON(Ac)CO -- Me                                                      3-1643 5 CON(Ac)CO -- Et                                                      3-1644 5 CON(Ac)CO -- Pr                                                      3-1645 5 CON(Ac)CO -- iPr                                                     3-1646 5 CON(Ac)CO -- Bu                                                      3-1647 5 CON(Ac)CO -- HOOCCH.sub.2 --                                         3-1648 5 CON(Ac)CO -- MeOOCCH.sub.2 --                                        3-1649 5 CON(Ac)CO -- MeCH(COOH)                                              3-1650 5 CON(Ac)CO -- HOOC--(CH.sub.2).sub.2 --                               3-1651 5 CON(Ac)CO -- MeCH(COOMe)                                             3-1652 5 CON(Ac)CO -- 1-HOOC-iBu                                              3-1653 5 CON(Ac)CO -- 1-MeOOC-iBu                                             3-1654 5 CON(Ac)CO -- 1-HOOC-iPn                                              3-1655 5 CON(Ac)CO -- 1-MeOOC-iPn                                             3-1656 5 CON(Ac)CO -- 1-HOOC-2-Me--Bu                                         3-1657 5 CON(Ac)CO -- 1-MeOOC-2-Me--Bu                                        3-1658 5 CON(ac)CO -- CH.sub.2 CH.sub.2 SO.sub.3 H                            3-1659 5 CON(Ac)CO -- Z-1                                                     3-1660 5 CON(Ac)CO -- Z-2                                                     3-1661 5 CON(Ac)CO -- Z-3                                                     3-1662 5 CON(Ac)CO -- Z-4                                                     3-1663 5 CON(Ac)CO -- Z-5                                                     3-1664 5 CON(Ac)CO -- Z-6                                                     3-1665 5 CON(Ac)CO -- Z-7                                                     3-1666 5 CON(Ac)CO -- Z-8                                                     3-1667 5 CON(Ac)CO -- Z-9                                                     3-1668 5 CON(Ac)CO -- Z-10                                                    3-1669 5 CON(Ac)CO -- Z-11                                                    3-1670 5 CON(Ac)CO -- Z-12                                                    3-1671 5 CON(Ac)CO -- 3-Py                                                    3-1672 5 CON(Ac)CO -- 4-Py                                                    3-1673 5 CONHCO NH H                                                          3-1674 5 CONHCO NH Ph                                                         3-1675 5 CONHCO NH 2-Me--Ph                                                   3-1676 5 CONHCO NH 4-Me--Ph                                                   3-1677 5 CONHCO NH 2,4-diMe--Ph                                               3-1678 5 CONHCO NH 3,4-diMe--Ph                                               3-1679 5 CONHCO NH 2-(CF.sub.3)Ph                                             3-1680 5 CONHCO NH 4-(CF.sub.3)Ph                                             3-1681 5 CONHCO NH 2-MeOPh                                                    3-1682 5 CONHCO NH 4-MeOPh                                                    3-1683 5 CONHCO NH 2-EtOPh                                                    3-1684 5 CONHCO NH 4-EtOPh                                                    3-1685 5 CONHCO NH 2-HOPh                                                     3-1686 5 CONHCO NH 4-HOPh                                                     3-1687 5 CONHCO NH 2-(HOOC)Ph                                                 3-1688 5 CONHCO MH 4-(HOOC)Ph                                                 3-1689 5 CONHCO nH 2-(MeOOC)Ph                                                3-1690 5 CONHCO NH 4-(MeOOC)Ph                                                3-1691 5 CONHCO NH 2-(EtOOC)Ph                                                3-1692 5 CONHCO NH 4-(EtOOC)Ph                                                3-1693 5 CONHCO NH 2-(tBuOOC)Ph                                               3-1694 5 CONHCO NH 4-(tBuOOC)Ph                                               3-1695 5 CONHCO NH 2-Cl--Ph                                                   3-1696 5 CONHCO NH 4-Cl--Ph                                                   3-1697 5 CONHCO NH 2-Br--Ph                                                   3-1698 5 CONHCO NH 4-Br--Ph                                                   3-1699 5 CONHCO NH 2-I--Ph                                                    3-1700 5 CONHCO NH 4-I--Ph                                                    3-1701 5 CONHCO NH 2-NO.sub.2 --Ph                                            3-1702 5 CONHCO NH 4-NO.sub.2 --Ph                                            3-1703 5 CONHCO NH 2-NH.sub.2 --Ph                                            3-1704 5 CONHCO NH 4-NH.sub.2 --Ph                                            3-1705 5 CONHCO NH 2-(HO.sub.3 S)Ph                                           3-1706 5 CONHCO NH 4-(HO.sub.3 S)Ph                                           3-1707 5 CONHCO NH 2-(NH.sub.2 O.sub.2 S)Ph                                   3-1708 5 CONHCO NH 4-(NH.sub.2 O.sub.2 S)Ph                                   3-1709 5 CONHCO NH 2-CN--Ph                                                   3-1710 5 CONHCO NH 4-CN--Ph                                                   3-1711 5 CONHCO NH 2-(HOCH.sub.2)Ph                                           3-1712 5 CONHCO NH 4-(HOCH.sub.2)Ph                                           3-1713 5 CONHCO NH Me                                                         3-1714 5 CONHCO NH Et                                                         3-1715 5 CONHCO NH Pr                                                         3-1716 5 CONHCO NH iPr                                                        3-1717 5 CONHCO NH Bu                                                         3-1718 5 CONHCO NH HOOCCH.sub.2 --                                            3-1719 5 CONHCO NH MeOOCCH.sub.2 --                                           3-1720 5 CONHCO NH MeCH(COOH)                                                 3-1721 5 CONHCO NH HOOC--(CH.sub.2).sub.2 --                                  3-1722 5 CONHCO NH MeCH(COOMe)                                                3-1723 5 CONHCO NH 1-HOOC-iBu                                                 3-1724 5 CONHCO NH 1-MeOOC-iBu                                                3-1725 5 CONHCO NH 1-HOOC-iPn                                                 3-1726 5 CONHCO NH 1-MeOOC-iPn                                                3-1727 5 CONHCO NH 1-HOOC-2-Me--Bu                                            3-1728 5 CONHOCO NH 1-MeOOC-2-Me--Bu                                          3-1729 5 CONHCO NH CH.sub.2 CH.sub.2 SO.sub.3 H                               3-1730 5 CONHCO NH HO                                                         3-1731 5 CONHCO NH MeO                                                        3-1732 5 CONHCO NH EtO                                                        3-1733 5 CONHCO NH Pro                                                        3-1734 5 CONHCO NH iPrO                                                       3-1735 5 CONHCO NH BuO                                                        3-1736 5 CONHOC NH iBuO                                                       3-1737 5 CONHCO NH sBuO                                                       3-1738 5 CONHCO NH tBuO                                                       3-1739 5 CONHOC NH HxO                                                        3-1740 5 CONHCO NH PhO                                                        3-1741 5 CONHCO NH BnO                                                        3-1742 5 CONHCO NH Z-1                                                        3-1744 5 CONHCO NH Z-3                                                        3-1745 5 CONHCO NH Z-4                                                        3-1748 5 CONHCO NH Z-5                                                        3-1747 5 CONHCO NH Z-6                                                        3-1748 5 CONHCO NH Z-7                                                        3-1749 5 CONHCO NH Z-8                                                        3-1750 5 CONHCO NH Z-9                                                        3-1751 5 CONHCO NH Z-10                                                       3-1752 5 CONHCO NH Z-11                                                       3-1753 5 CONHCO NH Z-12                                                       3-1754 5 CONHCO NH 3-Py                                                       3-1755 5 CONHCO NH 4-Py                                                       3-1756 5 CONHSO.sub.2 -- H                                                    3-1757 5 CONHSO.sub.2 -- Ph                                                   3-1758 5 CONHSO.sub.2 -- 2-Me--Ph                                             3-1759 5 CONHSO.sub.2 -- 4-Me--Ph                                             3-1760 5 CONHSO.sub.2 -- 2,4-diMe--Ph                                         3-1761 5 CONHSO.sub.2 -- 3,4-diMe--Ph                                         3-1762 5 CONHSO.sub.2 -- 2-(CF.sub.3)Ph                                       3-1763 5 CONHSO.sub.2 -- 4-(CF.sub.3)Ph                                       3-1764 5 CONHSO.sub.2 -- 2-MeOPh                                              3-1765 5 CONHSO.sub.2 -- 4-MeOPh                                              3-1766 5 CONHSO.sub.2 -- 2-EtOPh                                              3-1767 5 CONHSO.sub.2 -- 4-EtOPh                                              3-1768 5 CONHSO.sub.2 -- 2-HOPh                                               3-1769 5 CONHSO.sub.2 -- 4-HOPh                                               3-1770 5 CONHSO.sub.2 -- 2-(HOOC)Ph                                           3-1771 5 CONHSO.sub.2 -- 4-(HOOC)Ph                                           3-1772 5 CONHSO.sub.2 -- 2-(MeOOC)Ph                                          3-1773 5 CONHSO.sub.2 -- 4-(MeOOC)Ph                                          3-1774 5 CONHSO.sub.2 -- 2-(EtOOC)Ph                                          3-1775 5 CONHSO.sub.2 -- 4-(EtOOC)Ph                                          3-1776 5 CONHSO.sub.2 -- 2-(tBuOOC)Ph                                         3-1777 5 CONHSO.sub.2 -- 4-(tBuOOC)Ph                                         3-1778 5 CONHSO.sub.2 -- 2-Cl--Ph                                             3-1779 5 CONHSO.sub.2 -- 4-Cl--Ph                                             3-1780 5 CONHSO.sub.2 -- 2-Br--Ph                                             3-1781 5 CONHSO.sub.2 -- 4-Br--Ph                                             3-1782 5 CONHSO.sub.2 -- 2-I--Ph                                              3-1783 5 CONHSO.sub.2 -- 4-I--Ph                                              3-1784 5 CONHSO.sub.2 -- 2-NO.sub.2 --Ph                                      3-1785 5 CONHSO.sub.2 -- 4-NO.sub.2 --Ph                                      3-1786 5 CONHSO.sub.2 -- 2-NH.sub.2 --Ph                                      3-1787 5 CONHSO.sub.2 -- 4-NH.sub.2 --Ph                                      3-1788 5 CONHSO.sub.2 -- 2-(HO.sub.3 S)Ph                                     3-1789 5 CONHSO.sub.2 -- 4-(HO.sub.3 S)Ph                                     3-1790 5 CONHSO.sub.2 -- 2-(NH.sub.2 O.sub.2 S)Ph                             3-1791 5 CONHSO.sub.2 -- 4-(NH.sub.2 O.sub.2 S)Ph                             3-1792 5 CONHSO.sub.2 -- 2-CN--Ph                                             3-1793 5 CONHSO.sub.2 -- 4-CN--Ph                                             3-1794 5 CONHSO.sub.2 -- 2-(HOCH.sub.2)Ph                                     3-1795 5 CONHSO.sub.2 -- 4-(HOCH.sub.2)Ph                                     3-1796 5 CONHSO.sub.2 -- Me                                                   3-1797 5 CONHSO.sub.2 -- Et                                                   3-1798 5 CONHSO.sub.2 -- Pr                                                   3-1799 5 CONHSO.sub.2 -- iPr                                                  3-1800 5 CONHSO.sub.2 -- Bu                                                   3-1801 5 CONHSO.sub.2 -- HOOCCH.sub.2 --                                      3-1802 5 CONHSO.sub.2 -- MeOOCCH.sub.2 --                                     3-1803 5 CONHSO.sub.2 -- MeCH(COOH)                                           3-1804 5 CONHSO.sub.2 -- HOOC--(CH.sub.2).sub.2 --                            3-1805 5 CONHSO.sub.2 -- MeCH(COOMe)                                          3-1806 5 CONHSO.sub.2 -- 1-HOOC-iBu                                           3-1807 5 CONHSO.sub.2 -- 1-MeOOC-iBu                                          3-1808 5 CONHSO.sub.2 -- 1-HOOC-iPn                                           3-1809 5 CONHSO.sub.2 -- 1-MeOOC-iPn                                          3-1810 5 CONHSO.sub.2 -- 1-HOOC-2-Me--Bu                                      3-1811 5 CONHSO.sub.2 -- 1-MeOOC-2-Me--Bu                                     3-1812 5 CONHSO.sub.2 -- CH.sub.2 CH.sub.2 SO.sub.3 H                         3-1813 5 CONHSO.sub.2 -- OH                                                   3-1814 5 CONHSO.sub.2 -- MeO                                                  3-1815 5 CONHSO.sub.2 -- EtO                                                  3-1816 5 CONHSO.sub.2 -- PrO                                                  3-1817 5 CONHSO.sub.2 -- iPrO                                                 3-1818 5 CONHSO.sub.2 -- BuO                                                  3-1819 5 CONHSO.sub.2 -- iBuO                                                 3-1820 5 CONHSO.sub.2 -- sBuO                                                 3-1821 5 CONHSO.sub.2 -- tBuO                                                 3-1822 5 CONHSO.sub.2 -- HxO                                                  3-1823 5 CONHSO.sub.2 -- PhO                                                  3-1824 5 CONHSO.sub.2 -- BnO                                                  3-1825 5 CONHSO.sub.2 -- Z-1                                                  3-1826 5 CONHSO.sub.2 -- Z-2                                                  3-1827 5 CONHSO.sub.2 -- Z-3                                                  3-1828 5 CONHSO.sub.2 -- Z-4                                                  3-1829 5 CONHSO.sub.2 -- Z-5                                                  3-1830 5 CONHSO.sub.2 -- Z-6                                                  3-1831 5 CONHSO.sub.2 -- Z-7                                                  3-1832 5 CONHSO.sub.2 -- Z-8                                                  3-1833 5 CONHSO.sub.2 -- Z-9                                                  3-1834 5 CONHSO.sub.2 -- Z-10                                                 3-1835 5 CONHSO.sub.2 -- Z-11                                                 3-1836 5 CONHSO.sub.2 -- Z-12                                                 3-1837 5 CONHSO.sub.2 -- 3-Py                                                 3-1838 5 CONHSO.sub.2 -- 4-Py                                                 3-1839 5 CONHSO.sub.2 NH H                                                    3-1840 5 CONHSO.sub.2 NH Ph                                                   3-1841 5 CONHSO.sub.2 NH 2-Me--Ph                                             3-1842 5 CONHSO.sub.2 NH 4-Me--Ph                                             3-1843 5 CONHSO.sub.2 NH 2,4-diMe--Ph                                         3-1844 5 CONHSO.sub.2 NH 3,4-diMe--Ph                                         3-1845 5 CONHSO.sub.2 NH 2-(CF.sub.3)Ph                                       3-1846 5 CONHSO.sub.2 NH 4-(CF.sub.3)Ph                                       3-1847 5 CONHSO.sub.2 NH 2-MeOPh                                              3-1848 5 CONHSO.sub.2 NH 4-MeOPh                                              3-1849 5 CONHSO.sub.2 NH 2-EtOPh                                              3-1850 5 CONHSO.sub.2 NH 4-EtOPh                                              3-1851 5 CONHSO.sub.2 NH 2-HOPh                                               3-1852 5 CONHSO.sub.2 NH 4-HOPh                                               3-1853 5 CONHSO.sub.2 NH 2-(HOOC)Ph                                           3-1854 5 CONHSO.sub.2 NH 4-(HOOC)Ph                                           3-1855 5 CONHSO.sub.2 NH 2-(MeOOC)Ph                                          3-1856 5 CONHSO.sub.2 NH 4-(MeOOC)Ph                                          3-1857 5 CONHSO.sub.2 NH 2-(EtOOC)Ph                                          3-1858 5 CONHSO.sub.2 NH 4-(EtOOC)Ph                                          3-1859 5 CONHSO.sub.2 NH 2-(tBuOOC)Ph                                         3-1860 5 CONHSO.sub.2 NH 4-(tBuOOC)Ph                                         3-1861 5 CONHSO.sub.2 NH 2-Cl--Ph                                             3-1862 5 CONHSO.sub.2 NH 4-Cl--Ph                                             3-1863 5 CONHSO.sub.2 NH 2-Br--Ph                                             3-1864 5 CONHSO.sub.2 NH 4-Br--Ph                                             3-1865 5 CONHSO.sub.2 NH 2-I--Ph                                              3-1866 5 CONHSO.sub.2 NH 4-I--Ph                                              3-1867 5 CONHSO.sub.2 NH 2-NO.sub.2 --Ph                                      3-1868 5 CONHSO.sub.2 NH 4-NO.sub.2 --Ph                                      3-1869 5 CONHSO.sub.2 NH 2-NH.sub.2 --Ph                                      3-1870 5 CONHSO.sub.2 NH 4-NH.sub.2 --Ph                                      3-1871 5 CONHSO.sub.2 NH 2-(HO.sub.3 S)Ph                                     3-1872 5 CONHSO.sub.2 NH 4-(HO.sub.3 S)Ph                                     3-1873 5 CONHSO.sub.2 NH 2-(NH.sub.2 O.sub.2 S)Ph                             3-1874 5 CONHSO.sub.2 NH 4-(NH.sub.2 O.sub.2 S)Ph                             3-1875 5 CONHSO.sub.2 NH 2-CN--Ph                                             3-1876 5 CONHSO.sub.2 NH 4-CN--Ph                                             3-1877 5 CONHSO.sub.2 NH 2-(HOCH.sub.2)Ph                                     3-1878 5 CONHSO.sub.2 NH 4-(HOCH.sub.2)Ph                                     3-1879 5 CONHSO.sub.2 NH Me                                                   3-1880 5 CONHSO.sub.2 NH Et                                                   3-1881 5 CONHSO.sub.2 NH Pr                                                   3-1882 5 CONHSO.sub.2 NH iPr                                                  3-1883 5 CONHSO.sub.2 NH Bu                                                   3-1884 5 CONHSO.sub.2 NH HOOCCH.sub.2 --                                      3-1885 5 CONHSO.sub.2 NH MeOOCCH.sub.2 --                                     3-1886 5 CONHSO.sub.2 NH MeCH(COOH)                                           3-1887 5 CONHSO.sub.2 NH HOOC--(CH.sub.2).sub.2 --                            3-1888 5 CONHSO.sub.2 NH MeCH(COOMe)                                          3-1889 5 CONHSO.sub.2 NH 1-HOOC-iBu                                           3-1890 5 CONHSO.sub.2 NH 1-MeOOC-iBu                                          3-1891 5 CONHSO.sub.2 NH 1-HOOC-iPn                                           3-1892 5 CONHSO.sub.2 NH 1-MeOOC-iPn                                          3-1893 5 CONHSO.sub.2 NH 1-HOOC-2-Me--Bu                                      3-1894 5 CONHSO.sub.2 NH 1-MeOOC-2-Me--Bu                                     3-1895 5 CONHSO.sub.2 NH CH.sub.2 CH.sub.2 SO.sub.3 H                         3-1896 5 CONHSO.sub.2 NH OH                                                   3-1897 5 CONHSO.sub.2 NH MeO                                                  3-1898 5 CONHSO.sub.2 NH EtO                                                  3-1899 5 CONHSO.sub.2 NH PrO                                                  3-1900 5 CONHSO.sub.2 NH iPrO                                                 3-1901 5 CONHSO.sub.2 NH BuO                                                  3-1902 5 CONHSO.sub.2 NH iBuO                                                 3-1903 5 CONHSO.sub.2 NH sBuO                                                 3-1904 5 CONHSO.sub.2 NH tBuO                                                 3-1905 5 CONHSO.sub.2 NH HxO                                                  3-1906 5 CONHSO.sub.2 NH PhO                                                  3-1907 5 CONHSO.sub.2 NH BnO                                                  3-1908 5 CONHSO.sub.2 NH Z-1                                                  3-1909 5 CONHSO.sub.2 NH Z-2                                                  3-1910 5 CONHSO.sub.2 NH Z-3                                                  3-1911 5 CONHSO.sub.2 NH Z-4                                                  3-1912 5 CONHSO.sub.2 NH Z-5                                                  3-1913 5 CONHSO.sub.2 NH Z-6                                                  3-1914 5 CONHSO.sub.2 NH Z-7                                                  3-1915 5 CONHSO.sub.2 NH Z-8                                                  3-1916 5 CONHSO.sub.2 NH Z-9                                                  3-1917 5 CONHSO.sub.2 NH Z-10                                                 3-1918 5 CONHSO.sub.2 NH Z-11                                                 3-1919 5 CONHSO.sub.2 NH Z-12                                                 3-1920 5 CONHSO.sub.2 NH 3-Py                                                 3-1921 5 CONHSO.sub.2 NH 4-Py                                                 3-1922 5 NHCO -- H                                                            3-1923 5 NHCO -- Ph                                                           3-1924 5 NHCO -- 2-Me--Ph                                                     3-1925 5 NHCO -- 4-Me--Ph                                                     3-1926 5 NHCO -- 2,4-diMe--Ph                                                 3-1927 5 NHCO -- 3,4-diMe--Ph                                                 3-1928 5 NHCO -- 2-(CF.sub.3)Ph                                               3-1929 5 NHOC -- 4-(CF.sub.3)Ph                                               3-1930 5 NHOC -- 2-MeOPh                                                      3-1931 5 NHCO -- 4-MeOPh                                                      3-1932 5 NHCO -- 2-EtOPh                                                      3-1933 5 NHCO -- 4-EtOPh                                                      3-1934 5 NHCO -- 2-HOPh                                                       3-1935 5 NHCO -- 4-HOPh                                                       3-1936 5 NHCO -- 2-(HOOC)Ph                                                   3-1937 5 NHCO -- 4-(HOOC)Ph                                                   3-1938 5 NHCO -- 2-(MeOOC)Ph                                                  3-1939 5 NHCO -- 4-(MeOOC)Ph                                                  3-1940 5 NHCO -- 2-(EtOOC)Ph                                                  3-1941 5 NHCO -- 4-(EtOOC)Ph                                                  3-1942 5 NHCO -- 2-(tBuOOC)Ph                                                 3-1943 5 NHCO -- 4-(tBuOOC)Ph                                                 3-1944 5 NHCO -- 2-Cl--Ph                                                     3-1945 5 NHCO -- 4-Cl--Ph                                                     3-1946 5 NHCO -- 2-Br--Ph                                                     3-1947 5 NHCO -- 4-Br--Ph                                                     3-1948 5 NHCO -- 2-I--Ph                                                      3-1949 5 NHCO -- 4-I--Ph                                                      3-1950 5 NHCO -- 2-NO.sub.2 --Ph                                              3-1951 5 NHCO -- 4-NO.sub.2 --Ph                                              3-1952 5 NHCO -- 2-NH.sub.2 --Ph                                              3-1953 5 NHCO -- 4-NH.sub.2 --Ph                                              3-1954 5 NHCO -- 2-(HO.sub.3 S)Ph                                             3-1955 5 NHCO -- 4-(HO.sub.3 S)Ph                                             3-1956 5 NHCO -- 2-(NH.sub.2 O.sub.2 S)Ph                                     3-1957 5 NHCO -- 4-(NH.sub.2 O.sub.2 S)Ph                                     3-1958 5 NHCO -- 2-CN--Ph                                                     3-1959 5 NHCO -- 4-CN--Ph                                                     3-1960 5 NHCO -- 2-(HOCH.sub.2)Ph                                             3-1961 5 NHCO -- 4-(HOCH.sub.2)Ph                                             3-1962 5 NHCO -- Me                                                           3-1963 5 NHCO -- Et                                                           3-1964 5 NHCO -- Pr                                                           3-1965 5 NHCO -- iPr                                                          3-1966 5 NHCO -- Bu                                                           3-1967 5 NHCO -- HOOCCH.sub.2 --                                              3-1968 5 NHCO -- MeOOCCH.sub.2 --                                             3-1969 5 NHCO -- MeCH(COOH)                                                   3-1970 5 NHCO -- HOOC--(CH.sub.2).sub.2 --                                    3-1971 5 NHCO -- MeCH(COOMe)                                                  3-1972 5 NHCO -- 1-HOOC-iBu                                                   3-1973 5 NHCO -- 1-HOOC-iPn                                                   3-1974 5 NHCO -- 1-HOOC-2-Me--Bu                                              3-1975 5 NHCO -- CH.sub.2 CH.sub.2 SO.sub.3 OH                                3-1976 5 NHCO -- MeO                                                          3-1977 5 NHCO -- EtO                                                          3-1978 5 NHCO -- PrO                                                          3-1979 5 NHCO -- Z-1                                                          3-1980 5 NHCO -- Z-2                                                          3-1981 5 NHCO -- Z-3                                                          3-1982 5 NHCO -- Z-4                                                          3-1983 5 NHCO -- Z-5                                                          3-1984 5 NHCO -- Z-6                                                          3-1985 5 NHCO -- Z-7                                                          3-1986 5 NHCO -- Z-8                                                          3-1987 5 NHCO -- Z-9                                                          3-1988 5 NHCO -- Z-10                                                         3-1989 5 NHCO -- Z-11                                                         3-1990 5 NHCO -- Z-12                                                         3-1991 5 NHCO -- 3-Py                                                         3-1992 5 NHCO -- 4-Py                                                         3-1993 5 NHCO NH H                                                            3-1994 5 NHCO NH Ph                                                           3-1995 5 NHCO NH 2-Me--Ph                                                     3-1996 5 NHCO NH 4-Me--Ph                                                     3-1997 5 NHCO NH 2,4-diMe--Ph                                                 3-1998 5 NHCO NH 3,4-diMe--Ph                                                 3-1999 5 NHCO NH 2-(CF.sub.3)Ph                                               3-2000 5 NHCO NH 4-(CF.sub.3)Ph                                               3-2001 5 NHCO NH 2-MeOPh                                                      3-2002 5 NHCO NH 4-MeOPh                                                      3-2003 5 NHCO NH 2-EtOPh                                                      3-2004 5 NHCO NH 4-EtOPh                                                      3-2005 5 NHCO NH 2-HOPh                                                       3-2006 5 NHCO NH 4-HOPh                                                       3-2007 5 NHCO NH 2-(HOOC)Ph                                                   3-2008 5 NHCO NH 4-(HOOC)Ph                                                   3-2009 5 NHCO NH 2-(MeOOC)Ph                                                  3-2010 5 NHCO NH 4-(MeOOC)Ph                                                  3-2011 5 NHCO NH 2-(EtOOC)Ph                                                  3-2012 5 NHCO NH 4-(EtOOC)Ph                                                  3-2013 5 NHCO NH 2-(tBuOOC)Ph                                                 3-2014 5 NHCO NH 4-(tBuOOC)Ph                                                 3-2015 5 NHCO NH 2-Cl--Ph                                                     3-2016 5 NHCO NH 4-Cl--Ph                                                     3-2018 5 NHCO NH 4-Br--Ph                                                     3-2019 5 NHCO NH 2-I--Ph                                                      3-2020 5 NHCO NH 4-I--Ph                                                      3-2021 5 NHCO NH 2-NO.sub.2 --Ph                                              3-2022 5 NHCO NH 4-NO.sub.2 --Ph                                              3-2023 5 NHCO NH 2-NH.sub.2 --Ph                                              3-2024 5 NHCO NH 4-NH.sub.2 --Ph                                              3-2025 5 NHCO NH 2-(HO.sub.3 S)Ph                                             3-2026 5 NHCO NH 4-(HO.sub.3 S)Ph                                             3-2027 5 NHCO NH 2-(NH.sub.2 O.sub.2 S)Ph                                     3-2028 5 NHCO NH 4-(NH.sub.2 O.sub.2 S)Ph                                     3-2029 5 NHCO NH 2-CN--Ph                                                     3-2030 5 NHCO NH 4-CN--Ph                                                     3-2031 5 NHCO NH 2-(HOCH.sub.2)Ph                                             3-2032 5 NHOC NH 4-(HOCH.sub.2)Ph                                             3-2033 5 NHCO NH Me                                                           3-2034 5 NHCO NH Et                                                           3-2035 5 NHCO NH Pr                                                           3-2036 5 NHCO NH iPr                                                          3-2037 5 NHCO NH Bu                                                           3-2038 5 NHCO NH HOOCCH.sub.2 --                                              3-2039 5 NHCO NH MeOOCCH.sub.2 --                                             3-2040 5 NHCO NH MeCH(COOH)                                                   3-2041 5 NHCO NH HOOC--(CH.sub.2).sub.2 --                                    3-2042 5 NHCO NH MeCH(COOMe)                                                  3-2043 5 NHCO NH 1-HOOC-iBu                                                   3-2044 5 NHCO NH 1-MeOOC-iBu                                                  3-2045 5 NHCO NH 1-HOOC-iPn                                                   3-2046 5 NHCO NH 1-MeOOC-iPn                                                  3-2047 5 NHOC NH 1-HOOC-2-Me--Bu                                              3-2048 5 NHCO NH 1-MeOOC-2-Me--Bu                                             3-2049 5 NHCO NH CH.sub.2 CH.sub.2 SO.sub.3 H                                 3-2050 5 NHCO NH OH                                                           3-2051 5 NHCO NH MeO                                                          3-2052 5 NHOC NH EtO                                                          3-2053 5 NHOC NH PrO                                                          3-2054 5 NHCO NH iPrO                                                         3-2055 5 NHCO NH BuO                                                          3-2056 5 NHCO NH iBuO                                                         3-2057 5 NHCO NH sBuO                                                         3-2058 5 NHCO NH tBuO                                                         3-2059 5 NHCO NH HxO                                                          3-2060 5 NHCO NH PhO                                                          3-2061 5 NHCO NH BnO                                                          3-2062 5 NHCO NH Z-1                                                          3-2063 5 NHCO NH Z-2                                                          3-2064 5 NHCO NH Z-3                                                          3-2065 5 NHCO NH Z-4                                                          3-2066 5 NHCO NH Z-5                                                          3-2067 5 NHCO NH Z-6                                                          3-2068 5 NHCO NH Z-7                                                          3-2069 5 NHCO NH Z-8                                                          3-2070 5 NHCO NH Z-9                                                          3-2071 5 NHCO NH Z-10                                                         3-2072 5 NHCO NH Z-11                                                         3-2073 5 NHCO NH Z-12                                                         3-2074 5 NHCO NH 3-Py                                                         3-2075 5 NHCO NH 4-Py                                                         3-2076 5 NHCO NMe Ph                                                          3-2077 5 NHCO NMe 2-Me--Ph                                                    3-2078 5 NHCO NMe 4-Me--Ph                                                    3-2079 5 NHCO NMe 2,4-diMe--Ph                                                3-2080 5 NHCO NMe 3,4-diMe--Ph                                                3-2081 5 NHCO NMe 2-(CF.sub.3)Ph                                              3-2082 5 NHCO NMe 4-(CF.sub.3)Ph                                              3-2083 5 NHCO NMe 2-MeOPh                                                     3-2084 5 NHCO NMe 4-MeOPh                                                     3-2085 5 NHCO NMe 2-EtOPh                                                     3-2086 5 NHCO NMe 4-EtOPh                                                     3-2087 5 NHCO NMe 2-HOPh                                                      3-2088 5 NHCO NMe 4-HOPh                                                      3-2089 5 NHOC NMe 2-(HOOC)Ph                                                  3-2090 5 NHCO NMe 4-(HOOC)Ph                                                  3-2091 5 NHCO NMe 2-(MeOOC)Ph                                                 3-2092 5 NHCO NMe 4-(MeOOC)Ph                                                 3-2093 5 NHCO NMe 2-(EtOOC)Ph                                                 3-2095 5 NHCO NMe 2-(tBuOOC)Ph                                                3-2096 5 NHCO NMe 4-(tBuOOC)Ph                                                3-2097 5 NHCO NMe 2-Cl--Ph                                                    3-2098 5 NHCO NMe 4-Cl--Ph                                                    3-2100 5 NHCO NMe 4-Br--Ph                                                    3-2101 5 NHOC NMe 2-I--Ph                                                     3-2102 5 NHCO NMe 4-I--Ph                                                     3-2103 5 NHCO NMe 2-NO.sub.2 --Ph                                             3-2104 5 NHCO NMe 4-NO.sub.2 --Ph                                             3-2105 5 NHCO NMe 2-NH.sub.2 --Ph                                             3-2106 5 NHCO NMe 4-NH.sub.2 --Ph                                             3-2107 5 NHCO NMe 2-(HO.sub.3 S)Ph                                            3-2108 5 NHCO NMe 4-(HO.sub.3 S)Ph                                            3-2109 5 NHCO NMe 2-(NH.sub.2 O.sub.2 S)Ph                                    3-2110 5 NHCO NMe 4-(NH.sub.2 O.sub.2 S)Ph                                    3-2111 5 NHCO NMe 2-CN--Ph                                                    3-2112 5 NHCO NMe 4-CN--Ph                                                    3-2113 5 NHCO NMe 2-(HOCH.sub.2)Ph                                            3-2114 5 NHCO NMe 4-(HOCH.sub.2)Ph                                            3-2115 5 NHCO NMe Me                                                          3-2116 5 NHCO NMe Et                                                          3-2117 5 NHCO NMe Pr                                                          3-2118 5 NHCO NMe iPr                                                         3-2119 5 NHCO NMe Bu                                                          3-2120 5 NHCO NMe HOOCCH.sub.2 --                                             3-2121 5 NHCO NMe MeOOCCH.sub.2 --                                            3-2122 5 NHCO NMe MeCH(COOH)                                                  3-2123 5 NHCO NMe HOOC--(CH.sub.2).sub.2 --                                   3-2124 5 NHCO NMe MeCH(COOMe)                                                 3-2125 5 NHCO NMe 1-HOOC-iBu                                                  3-2126 5 NHCO NMe 1-MeOOC-iBu                                                 3-2127 5 NHCO NMe 1-HOOC-iPn                                                  3-2128 5 NHCO NMe 1-MeOOC-iPn                                                 3-2129 5 NHCO NMe 1-HOOC-2-Me--Bu                                             3-2130 5 NHCO NMe 1-MeOOC-2-Me--Bu                                            3-2131 5 NHCO NMe CH.sub.2 CH.sub.2 SO.sub.3 H                                3-2132 5 NHCO NMe OH                                                          3-2133 5 NHCO NMe MeO                                                         3-2134 5 NHCO NMe EtO                                                         3-2135 5 NHCO NMe PrO                                                         3-2136 5 NHCO NMe iPrO                                                        3-2137 5 NHCO NMe BuO                                                         3-2138 5 NHCO NMe iBuO                                                        3-2139 5 NHCO NMe sBuO                                                        3-2140 5 NHCO NMe tBuO                                                        3-2141 5 NHCO NMe HxO                                                         3-2142 5 NHCO NMe PhO                                                         3-2143 5 NHCO NMe BnO                                                         3-2144 5 NHCO NMe Z-1                                                         3-2145 5 NHCO NMe Z-2                                                         3-2147 5 NHCO NMe Z-3                                                         3-2147 5 NHCO NMe Z-4                                                         3-2148 5 NHCO NMe Z-5                                                         3-2149 5 NHCO NMe Z-6                                                         3-2150 5 NHCO NMe Z-7                                                         3-2151 5 NHCO NMe Z-8                                                         3-2152 5 NHCO NMe Z-9                                                         3-2153 5 NHCO NMe Z-10                                                        3-2154 5 NHCO NMe Z-11                                                        3-2155 5 NHCO NMe Z-12                                                        3-2156 5 NHCO NMe 3-Py                                                        3-2157 5 NHCO NMe 4-Py                                                      3-2158                                                                              5     NHCO         NHNH   H                                               3-2159 5 NHCO NHNH Me                                                         3-2160 5 NHCO NHNH Et                                                         3-2161 5 NHCO NHNMe Me                                                        3-2162 5 NHCO NHNMe Et                                                        3-2163 5 NHCO NHNMe Pr                                                      3-2164                                                                              5     NHCONHNHCO     NH   H                                               3-2165 5 NHCONHNHCO NH Ph                                                     3-2166 5 NHCONHNHCO NH 2-Me--Ph                                               3-2167 5 NHCONHNHCO NH 4-Me--Ph                                               3-2168 5 NHCONHNHCO NH 2,4-diMe--Ph                                           3-2169 5 NHCONHNHCO NH 3,4-diMe--Ph                                           3-2170 5 NHCONHNHCO NH 2-(CF.sub.3)Ph                                         3-2171 5 NHCONHNHCO NH 4-(CF.sub.3)Ph                                         3-2172 5 NHCONHNHCO NH 2-MeOPh                                                3-2173 5 NHCONHNHCO NH 4-MeOPh                                                3-2174 5 NHCONHNHCO NH 2-EtOPh                                                3-2175 5 NHCONHNHCO NH 4-EtOPh                                                3-2176 5 NHCONHNHCO NH 2-HOPh                                                 3-2177 5 NHCONHNHCO NH 4-HOPh                                                 3-2178 5 NHCONHNHCO NH 2-(HOOC)Ph                                             3-2179 5 NHCONHNHCO NH 4-(HOOC)Ph                                             3-2180 5 NHCONHNHCO NH 2-(MeOOC)Ph                                            3-2181 5 NHCONHNHCO NH 4-(MeOOC)Ph                                            3-2182 5 NHCONHNHCO NH 2-(EtOOC)Ph                                            3-2183 5 NHCONHNHCO NH 4-(EtOOC)Ph                                            3-2184 5 NHCONHNHCO NH 2-(tBuOOC)Ph                                           3-2185 5 NHCONHNHCO NH 4-(tBuOOC)Ph                                           3-2186 5 NHCONHNHCO NH 2-Cl--Ph                                               3-2187 5 NHCONHNHCO NH 4-Cl--Ph                                               3-2188 5 NHCONHNHCO NH 2-Br--Ph                                               3-2189 5 NHCONHNHCO NH 4-Br--Ph                                               3-2190 5 NHCONHNHCO NH 2-I--Ph                                                3-2191 5 NHCONHNHCO NH 4-I--Ph                                                3-2192 5 NHCONHNHCO NH 2-NO.sub.2 --Ph                                        3-2193 5 NHCONHNHCO NH 4-NO.sub.2 --Ph                                        3-2194 5 NHCONHNHCO NH 2-NH.sub.2 --Ph                                        3-2195 5 NHCONHNHCO NH 4-NH.sub.2 --Ph                                        3-2196 5 NHCONHNHCO NH 2-(HO.sub.3 S)Ph                                       3-2197 5 NHCONHNHCO NH 4-(HO.sub.3 S)Ph                                       3-2198 5 NHCONHNHCO NH 2-(NH.sub.2 O.sub.2 S)Ph                               3-2199 5 NHCONHNHCO NH 4-(NH.sub.2 O.sub.2 S)Ph                               3-2200 5 NHCONHNHCO NH 2-CN--Ph                                               3-2201 5 NHCONHNHCO NH 4-CN--Ph                                               3-2202 5 NHCONHNHCO NH 2-(HOCH.sub.2)Ph                                       3-2203 5 NHCONHNHCO NH 4-(HOCH.sub.2)Ph                                       3-2204 5 NHCONHNHCO NH Me                                                     3-2205 5 NHCONHNHCO NH Et                                                     3-2206 5 NHCONHNHCO NH Pr                                                     3-2207 5 NHCONHNHCO NH iPr                                                    3-2208 5 NHCONHNHCO NH Bu                                                     3-2209 5 NHCONHNHCO NH HOOCCH.sub.2 --                                        3-2210 5 NHCONHNHCO NH MeOOCCH.sub.2 --                                       3-2211 5 NHCONHNHCO NH MeCH(COOH)                                             3-2212 5 NHCONHNHCO NH HOOC--(CH.sub.2).sub.2 --                              3-2213 5 NHCONHNHCO NH MeCH(COOMe)                                            3-2214 5 NHCONHNHCO NH 1-HOOC-iBu                                             3-2215 5 NHCONHNHCO NH 1-MeOOC-iBu                                            3-2216 5 NHCONHNHCO NH 1-HOOC-iPn                                             3-2217 5 NHCONHNHCO NH 1-MeOOC-iPn                                            3-2218 5 NHCONHNHCO NH 1-HOOC-2-Me--Bu                                        3-2219 5 NHCONHNHCO NH 1-MeOOC-2-Me--Bu                                       3-2220 5 NHCONHNHCO NH CH.sub.2 CH.sub.2 SO.sub.3 H                           3-2221 5 NHCONHNHCO NH OH                                                     3-2222 5 NHCONHNHCO NH MeO                                                    3-2223 5 NHCONHNHCO NH EtO                                                    3-2224 5 NHCONHNHCO NH PrO                                                    3-2225 5 NHCONHNHCO NH iPrO                                                   3-2226 5 NHCONHNHCO NH BuO                                                    3-2227 5 NHCONHNHCO NH iBuO                                                   3-2228 5 NHCONHNHCO NH sBuO                                                   3-2229 5 NHCONHNHCO NH tBuO                                                   3-2230 5 NHCONHNHCO NH Hxo                                                    3-2231 5 NHCONHNHCO NH PhO                                                    3-2232 5 NHCONHNHCO NH BnO                                                    3-2233 5 NHCONHNHCO NH Z-1                                                    3-2234 5 NHCONHNHCO NH Z-2                                                    3-2235 5 NHCONHNHCO NH Z-3                                                    3-2236 5 NHCONHNHCO NH Z-4                                                    3-2237 5 NHCONHNHCO NH Z-5                                                    3-2238 5 NHCONHNHCO NH Z-6                                                    3-2239 5 NHCONHNHCO NH Z-7                                                    3-2240 5 NHCONHNHCO NH Z-8                                                    3-2241 5 NHCONHNHCO NH Z-9                                                    3-2242 5 NHCONHNHCO NH Z-10                                                   3-2243 5 NHCONHNHCO NH Z-11                                                   3-2244 5 NHCONHNHCO NH Z-12                                                   3-2245 5 NHCONHNHCO NH 3-Py                                                   3-2246 5 NHCONHNHCO  NH 4-Py                                                  3-2247 5 NHCONHCO -- H                                                        3-2248 5 NHCONHCO -- Ph                                                       3-2249 5 NHCONHCO -- 2-Me--Ph                                                 3-2250 5 NHCONHCO -- 4-Me--Ph                                                 3-2251 5 NHCONHCO -- 2,4-diMe--Ph                                             3-2252 5 NHCONHCO -- 3,4-diMe--Ph                                             3-2253 5 NHCONHCO -- 2-(CF.sub.3)Ph                                           3-2254 5 NHCONHCO -- 4-(CF.sub.3)Ph                                           3-2255 5 NHCONHCO -- 2-MeOPh                                                  3-2256 5 NHCONHCO -- 4-MeOPh                                                  3-2257 5 NHCONHCO -- 2-EtOPh                                                  3-2258 5 NHCONHCO -- 4-EtOPh                                                  3-2259 5 NHCONHCO -- 2-HOPh                                                   3-2260 5 NHCONHCO -- 4-HOPh                                                   3-2261 5 NHCONHCO -- 2-(HOOC)Ph                                               3-2262 5 NHCONHCO -- 4-(HOOC)Ph                                               3-2263 5 NHCONHCO -- 2-(MeOOC)Ph                                              3-2264 5 NHCONHCO -- 4-(MeOOC)Ph                                              3-2265 5 NHCONHCO -- 2-(EtOOC)Ph                                              3-2266 5 NHCONHCO -- 4-(EtOOC)Ph                                              3-2267 5 NHCONHCO -- 2-(tBuOOC)Ph                                             3-2268 5 NHCONHCO -- 4-(tBuOOC)Ph                                             3-2269 5 NHCONHCO -- 2-Cl--Ph                                                 3-2270 5 NHCONHCO -- 4-Cl--Ph                                                 3-2271 5 NHCONHCO -- 2-Br--Ph                                                 3-2272 5 NHCONHCO -- 4-Br--Ph                                                 3-2273 5 NHCONHCO -- 2-I--Ph                                                  3-2274 5 NHCONHCO -- 4-I--Ph                                                  3-2275 5 NHCONHCO -- 2-NO.sub.2 --Ph                                          3-2276 5 NHCONHCO -- 4-NO.sub.2 --Ph                                          3-2277 5 NHCONHCO -- 2-NH.sub.2 --Ph                                          3-2278 5 NHCONHCO -- 4-NH.sub.2 --Ph                                          3-2279 5 NHCONHCO -- 2-(HO.sub.3 S)Ph                                         3-2280 5 NHCONHCO -- 4-(HO.sub.3 S)Ph                                         3-2281 5 NHCONHCO -- 2-(NH.sub.2 O.sub.2 S)Ph                                 3-2282 5 NHCONHCO -- 4-(NH.sub.2 O.sub.2 S)Ph                                 3-2283 5 NHCONHCO -- 2-CN--Ph                                                 3-2284 5 NHCONHCO -- 4-CN--Ph                                                 3-2285 5 NHCONHCO -- 2-(HOCH.sub.2)Ph                                         3-2286 5 NHCONHCO -- 4-(HOCH.sub.2)Ph                                         3-2287 5 NHCONHCO -- Me                                                       3-2288 5 NHCONHCO -- Et                                                       3-2289 5 NHCONHCO -- Pr                                                       3-2290 5 NHCONHCO -- iPr                                                      3-2291 5 NHCONHCO -- Bu                                                       3-2292 5 NHCONHCO -- HOOCCH.sub.2 --                                          3-2293 5 NHCONHCO -- MeOOCCH.sub.2 --                                         3-2294 5 NHCONHCO -- MeCH(COOH)                                               3-2295 5 NHCONHCO -- HOOC--(CH.sub.2).sub.2 --                                3-2296 5 NHCONHCO -- MeCH(COOMe)                                              3-2297 5 NHCONHCO -- 1-HOOC-iBu                                               3-2298 5 NHCONHCO -- 1-MeOOC-iBu                                              3-2299 5 NHCONHCO -- 1-HOOC-iPn                                               3-2300 5 NHCONHCO -- 1-MeOOC-iPn                                              3-2301 5 NHCONHCO -- 1-HOOC-2-Me--Bu                                          3-2302 5 NHCONHCO -- 1-MeOOC-2-Me--Bu                                         3-2303 5 NHCONHCO -- CH.sub.2 CH.sub.2 SO.sub.3 H                             3-2304 5 NHCONHCO -- MeO                                                      3-2305 5 NHCONHCO -- EtO                                                      3-2306 5 NHCONHCO -- PrO                                                      3-2307 5 NHCONHCO -- iPrO                                                     3-2308 5 NHCONHCO -- BuO                                                      3-2309 5 NHCONHCO -- iBuO                                                     3-2310 5 NHCONHCO -- sBuO                                                     3-2311 5 NHCONHCO -- tBuO                                                     3-2312 5 NHCONHCO -- HxO                                                      3-2313 5 NHCONHCO -- PhO                                                      3-2314 5 NHCONHCO -- BnO                                                      3-2315 5 NHCONHCO -- Z-1                                                      3-2316 5 NHCONHCO -- Z-2                                                      3-2317 5 NHCONHCO -- Z-3                                                      3-2318 5 NHCONHCO -- Z-4                                                      3-2319 5 NHCONHCO -- Z-5                                                      3-2320 5 NHCONHCO -- Z-6                                                      3-2321 5 NHCONHCO -- Z-7                                                      3-2322 5 NHCONHCO -- Z-8                                                      3-2323 5 NHCONHCO -- Z-9                                                      3-2324 5 NHCONHCO -- Z-10                                                     3-2325 5 NHCONHCO -- Z-11                                                     3-2326 5 NHCONHCO -- Z-12                                                     3-2327 5 NHCONHCO -- 3-Py                                                     3-2328 5 NHCONHCO -- 4-Py                                                     3-2329 5 NHCONHSO.sub.2 -- H                                                  3-2330 5 NHCONHSO.sub.2 -- Ph                                                 3-2331 5 NHCONHSO.sub.2 -- 2-Me--Ph                                           3-2332 5 NHCONHSO.sub.2 -- 4-Me--Ph                                           3-2333 5 NHCONHSO.sub.2 -- 2,4-diMe--Ph                                       3-2334 5 NHCONHSO.sub.2 -- 3,4-diMe--Ph                                       3-2335 5 NHCONHSO.sub.2 -- 2-(CF.sub.3)Ph                                     3-2336 5 NHCONHSO.sub.2 -- 4-(CF.sub.3)Ph                                     3-2337 5 NHCONHSO.sub.2 -- 2-MeOPh                                            3-2338 5 NHCONHSO.sub.2 -- 4-MeOPh                                            3-2339 5 NHCONHSO.sub.2 -- 2-EtOPh                                            3-2340 5 NHCONHSO.sub.2 -- 4-EtOPh                                            3-2341 5 NHCONHSO.sub.2 -- 2-HOPh                                             3-2342 5 NHCONHSO.sub.2 -- 4-HOPh                                             3-2343 5 NHCONHSO.sub.2 -- 2-(HOOC)Ph                                         3-2344 5 NHCONHSO.sub.2 -- 4-(HOOC)Ph                                         3-2345 5 NHCONHSO.sub.2 -- 2-(MeOOC)Ph                                        3-2346 5 NHCONHSO.sub.2 -- 4-(MeOOC)Ph                                        3-2347 5 NHCONHSO.sub.2 -- 2-(EtOOC)Ph                                        3-2348 5 NHCONHSO.sub.2 -- 4-(EtOOC)Ph                                        3-2349 5 NHCONHSO.sub.2 -- 2-(tBuOOC)Ph                                       3-2350 5 NHCONHSO.sub.2 -- 4-(tBuOOC)Ph                                       3-2351 5 NHCONHSO.sub.2 -- 2-Cl--Ph                                           3-2352 5 NHCONHSO.sub.2 -- 4-Cl--Ph                                           3-2353 5 NHCONHSO.sub.2 -- 2-Br--Ph                                           3-2354 5 NHCONHSO.sub.2 -- 4-Br--Ph                                           3-2355 5 NHCONHSO.sub.2 -- 2-I--Ph                                            3-2356 5 NHCONHSO.sub.2 -- 4-I--Ph                                            3-2357 5 NHCONHSO.sub.2 -- 2-NO.sub.2 --Ph                                    3-2358 5 NHCONHSO.sub.2 -- 4-NO.sub.2 --Ph                                    3-2359 5 NHCONHSO.sub.2 -- 2-NH.sub.2 --Ph                                    3-2360 5 NHCONHSO.sub.2 -- 4-NH.sub.2 --Ph                                    3-2361 5 NHCONHSO.sub.2 -- 2-(HO.sub.3 S)Ph                                   3-2362 5 NHCONHSO.sub.2 -- 4-(HO.sub.3 S)Ph                                   3-2363 5 NHCONHSO.sub.2 -- 2-(NH.sub.2 O.sub.2 S)Ph                           3-2364 5 NHCONHSO.sub.2 -- 4-(NH.sub.2 O.sub.2 S)Ph                           3-2365 5 NHCONHSO.sub.2 -- 2-CN--Ph                                           3-2366 5 NHCONHSO.sub.2 -- 4-CN--Ph                                           3-2367 5 NHCONHSO.sub.2 -- 2-(HOCH.sub.2)Ph                                   3-2368 5 NHCONHSO.sub.2 -- 4-(HOCH.sub.2)Ph                                   3-2369 5 NHCONHSO.sub.2 -- Me                                                 3-2370 5 NHCONHSO.sub.2 -- Et                                                 3-2371 5 NHCONHSO.sub.2 -- Pr                                                 3-2372 5 NHCONHSO.sub.2 -- iPr                                                3-2373 5 NHCONHSO.sub.2 -- Bu                                                 3-2374 5 NHCONHSO.sub.2 -- HOOCCH.sub.2                                       3-2375 5 NHCONHSO.sub.2 -- MeOOCCH.sub.2                                      3-2376 5 NHCONHSO.sub.2 -- MeCH(COOH)                                         3-2377 5 NHCONHSO.sub.2 -- HOOC--(CH.sub.2).sub.2                             3-2378 5 NHCONHSO.sub.2 -- MeCH(COOMe)                                        3-2379 5 NHCONHSO.sub.2 -- 1-HOOC-iBu                                         3-2380 5 NHCONHSO.sub.2 -- 1-MeOOC-iBu                                        3-2381 5 NHCONHSO.sub.2 -- 1-HOOC-iPn                                         3-2382 5 NHCONHSO.sub.2 -- 1-MeOOC-iPn                                        3-2383 5 NHCONHSO.sub.2 -- 1-HOOC-2-Me--Bu                                    3-2384 5 NHCONHSO.sub.2 -- 1-MeOOC-2-Me--Bu                                   3-2385 5 NHCONHSO.sub.2 -- CH.sub.2 CH.sub.2 SO.sub.3 H                       3-2386 5 NHCONHSO.sub.2 -- OH                                                 3-2387 5 NHCONHSO.sub.2 -- MeO                                                3-2388 5 NHCONHSO.sub.2 -- EtO                                                3-2389 5 NHCONHSO.sub.2 -- Pro                                                3-2390 5 NHCONHSO.sub.2 -- iPrO                                               3-2391 5 NHCONHSO.sub.2 -- BuO                                                3-2392 5 NHCONHSO.sub.2 -- iBuO                                               3-2393 5 NHCONHSO.sub.2 -- sBuO                                               3-2394 5 NHCONHSO.sub.2 -- tBuO                                               3-2395 5 NHCONHSO.sub.2 -- HxO                                                3-2396 5 NHCONHSO.sub.2 -- PhO                                                3-2397 5 NHCONHSO.sub.2 -- Bno                                                3-2398 5 NHCONHSO.sub.2 -- Z-1                                                3-2399 5 NHCONHSO.sub.2 -- Z-2                                                3-2400 5 NHCONHSO.sub.2 -- Z-3                                                3-2401 5 NHCONHSO.sub.2 -- Z-4                                                3-2402 5 NHCONHSO.sub.2 -- Z-5                                                3-2403 5 NHCONHSO.sub.2 -- Z-6                                                3-2404 5 NHCONHSO.sub.2 -- Z-7                                                3-2405 5 NHCONHSO.sub.2 -- Z-8                                                3-2406 5 NHCONHSO.sub.2 -- Z-9                                                3-2407 5 NHCONHSO.sub.2 -- Z-10                                               3-2408 5 NHCONHSO.sub.2 -- Z-11                                               3-2409 5 NHCONHSO.sub.2 -- Z-12                                               3-2410 5 NHCONHSO.sub.2 -- 3-Py                                               3-2411 5 NHCONHSO.sub.2 -- 4-Py                                               3-2412 5 NHCONHSO.sub.2 NH H                                                  3-2413 5 NHCONHSO.sub.2 NH Me                                                 3-2414 5 NHCONHSO.sub.2 NH Et                                                 3-2415 5 NHCONHSO.sub.2 NH  Pr                                                3-2416 5 NHCONHSO.sub.2 NH iPr                                                3-2417 5 NHCONHSO.sub.2 NH Bu                                                 3-2418 5 NHCONHSO.sub.2 NMe Me                                                3-2419 5 NHCONHSO.sub.2 NMe Et                                                3-2420 5 NHCONHSO.sub.2 NMe Pr                                                3-2421 5 NHCONHSO.sub.2 NMe iPr                                               3-2422 5 NHCONHSO.sub.2 NMe Bu                                                3-2423 5 -- NH H                                                              3-2424 5 -- NH  Me                                                            3-2425 5 -- NH Et                                                             3-2426 5 -- NH Pr                                                             3-2427 5 -- NH iPr                                                            3-2428 5 -- NH Bu                                                           3-2429                                                                              5     CO             Pyr                                                  3-2430 5 CO Pipri                                                             3-2431 5 CO Pipra                                                             3-2432 5 CO Mor                                                               3-2433 5 CO Thmor                                                             3-2434 5 CO NHPyr                                                             3-2435 5 CO NHPipri                                                           3-2436 5 CO NHPipra                                                           3-2437 5 CO NHMor                                                             3-2438 5 CO NHThmor                                                           3-2439 5 NHCO Pyr                                                             3-2440 5 NHCO Pipri                                                           3-2441 5 NHCO Pipra                                                           3-2442 5 NHCO Mor                                                             3-2443 5 NHCO Thmor                                                           3-2444 5 NHCO NHPyr                                                           3-2445 5 NHCO NHPipri                                                         3-2446 5 NHCO NHPipra                                                         3-2447 5 NHCO NHMor                                                           3-2448 5 NHCO NHThmor                                                         3-2449 5 CONHCO Pyr                                                           3-2450 5 CONHCO Pipri                                                         3-2451 5 CONHCO Pipra                                                         3-2452 5 CONHCO Mor                                                           3-2453 5 CONHCO Thmor                                                         3-2454 5 CONHCO NHPyr                                                         3-2455 5 CONHCO NHPipri                                                       3-2456 5 CONHCO NHPipra                                                       3-2457 5 CONHCO NHMor                                                         3-2458 5 CONHCO NHThmor                                                       3-2459 5 CONHSO.sub.2 Pyr                                                     3-2460 5 CONHSO.sub.2 Pipri                                                   3-2461 5 CONHSO.sub.2 Pipra                                                   3-2462 5 CONHSO.sub.2 Mor                                                     3-2463 5 CONHSO.sub.2 Thmor                                                   3-2464 5 CONHSO.sub.2 NHPyr                                                   3-2465 5 CONHSO.sub.2 NHPipri                                                 3-2466 5 CONHSO.sub.2 NHPipra                                                 3-2467 5 CONHSO.sub.2 NHMor                                                   3-2468 5 CONHSO.sub.2 NHThmor                                               3-2469                                                                              5     NHSO.sub.2     NH   Z-4                                             3-2470 5 NHSO.sub.2 -- Me                                                     3-2471 5 NHSO.sub.2 -- Et                                                     3-2472 5 NHSO.sub.2 -- Pr                                                     3-2473 5 NHSO.sub.2 -- CH.sub.2 --Cl                                          3-2474 5 NHSO.sub.2 -- Ph                                                     3-2475 5 NHSO.sub.2 -- 4-Me--Ph                                               3-2476 5 CO NMe Ph                                                            3-2477 5 CO NMe 2-Me--Ph                                                      3-2478 5 CO NMe 4-Me--Ph                                                      3-2479 5 CO NMe 2,4-diMe--Ph                                                  3-2480 5 CO NMe 3,4-diMe--Ph                                                  3-2481 5 CO NMe 2-(CF.sub.3)Ph                                                3-2482 5 CO NMe 4-(CF.sub.3)Ph                                                3-2483 5 CO NMe 2-MeOPh                                                       3-2484 5 CO NMe 4-MeOPh                                                       3-2485 5 CO NMe 2-EtOPh                                                       3-2486 5 CO NMe 4-EtOPh                                                       3-2487 5 CO NMe 2-HOPh                                                        3-2488 5 CO NMe 4-HOPh                                                        3-2489 5 CO NMe 2-(HOOC)Ph                                                    3-2490 5 CO NMe 4-(HOOC)Ph                                                    3-2491 5 CO NMe 2-(MeOOC)Ph                                                   3-2492 5 CO NMe 4-(MeOOC)Ph                                                   3-2493 5 CO NMe 2-(EtOOC)Ph                                                   3-2494 5 CO NMe 4-(EtOOC)Ph                                                   3-2495 5 CO NMe 2-(tBuOOC)Ph                                                  3-2496 5 CO NMe 4-(tBuOOC)Ph                                                  3-2497 5 CO NMe 2-Cl--Ph                                                      3-2498 5 CO NMe 4-Cl--Ph                                                      3-2499 5 CO NMe 2-Br--Ph                                                      3-2500 5 CO NMe 4-Br--Ph                                                      3-2501 5 CO NMe 2-I--Ph                                                       3-2502 5 CO NMe 4-I--Ph                                                       3-2503 5 CO NMe 2-NO.sub.2 --Ph                                               3-2504 5 CO NMe 4-NO.sub.2 --Ph                                               3-2505 5 CO NMe 2-NH.sub.2 --Ph                                               3-2506 5 CO NMe 4-NH.sub.2 --Ph                                               3-2507 5 CO NMe 2-(HO.sub.3 S)Ph                                              3-2508 5 CO NMe 4-(HO.sub.3 S)Ph                                              3-2509 5 CO NMe 2-(NH.sub.2 O.sub.2 S)Ph                                      3-2510 5 CO NMe 4-(NH.sub.2 O.sub.2 S)Ph                                      3-2511 5 CO NMe 2-CN--Ph                                                      3-2512 5 CO NMe 4-CN--Ph                                                      3-2513 5 CO NMe 2-(HOCH.sub.2)Ph                                              3-2514 5 CO NMe 4-(HOCH.sub.2)Ph                                              3-2515 5 CO NMe Me                                                            3-2516 5 CO NMe Et                                                            3-2517 5 CO NMe Pr                                                            3-2518 5 CO NMe iPr                                                           3-2519 5 CO NMe Bu                                                            3-2520 5 CO NMe HOOCCH.sub.2                                                  3-2521 5 CO NMe HOOC--(CH.sub.2).sub.2                                        3-2522 5 CO NMe MeCH(COOH)                                                    3-2523 5 CO NMe HOOC--(CH.sub.2).sub.3 --                                     3-2524 5 CO NMe MeCH(COOMe)                                                   3-2525 5 CO NMe 1-HOOC-iBu                                                    3-2526 5 CO NMe 1-MeOOC-iBu                                                   3-2527 5 CO NMe 1-HOOC-iPn                                                    3-2528 5 CO NMe 1-MeOOC-iPn                                                   3-2529 5 CO Nme 1-HOOC-2-Me--Bu                                               3-2530 5 CO NMe 1-MeOOC-2-Me--Bu                                              3-2531 5 CO NMe CH.sub.2 CH.sub.2 SO.sub.3 H                                  3-2532 5  CO NMe OH                                                           3-2533 5 CO NMe MeO                                                           3-2534 5 CO NMe EtO                                                           3-2535 5 CO  NMe Pro                                                          3-2536 5 CO NMe iPrO                                                          3-2537 5  CO NMe BuO                                                          3-2538 5 CO NMe iBuO                                                          3-2539 5 CO NMe sBuO                                                          3-2540 5 CO NMe tBuO                                                          3-2541 5 CO NMe HxO                                                           3-2542 5 CO NMe PhO                                                           3-2543 5 CO NMe BnO                                                           3-2544 5 CO NMe Z-1                                                           3-2545 5 CO NMe Z-2                                                           3-2546 5 CO NMe Z-3                                                           3-2547 5 CO NMe Z-4                                                           3-2548 5 CO NMe Z-5                                                           3-2549 5 CO NMe Z-6                                                           3-2550 5 CO NMe Z-7                                                           3-2551 5 CO NMe Z-8                                                           3-2552 5 CO NMe Z-9                                                           3-2553 5 CO NMe Z-10                                                          3-2554 5 CO NMe Z-11                                                          3-2555 5 CO NMe Z-12                                                          3-2556 5 CO NMe 3-Py                                                          3-2557 5 CO NMe 4-Py                                                        3-2558                                                                              5     CO             Thiad                                                3-2559 5 CO NHThiad                                                           3-2560 5 NHCO Thiad                                                           3-2561 5 NHCO NHThiad                                                         3-2562 5 CONHCO Thiad                                                         3-2563 5 CONHCO NHThiad                                                       3-2564 5 CONHSO.sub.2 Thiad                                                   3-2565 5 CONHSO.sub.2 NHThiad                                               3-2566                                                                              5     NHCS           NH   H                                               3-2567 5 NHCS NH Me                                                           3-2568 5 NHCS NH Et                                                           3-2569 5 NHCS NH Ph                                                           3-2570 5 NHCS NH HOOCCH.sub.2                                                 3-2571 5 NHCS NH MeOOCCH.sub.2                                                3-2572 5 NHCS NH MeCH(COOH)                                                   3-2573 5 NHC S NH HOOC--(CH.sub.2).sub.2                                      3-2574 5 NHCS NH MeCH(COOMe)                                                  3-2575 5 CO NH HOOC--(CH.sub.2).sub.3 --                                      3-2576 5 NHCO NH HOOC--(CH.sub.2).sub.3 --                                    3-2577 5 NHCO -- HOOC--(CH.sub.2).sub.3 --                                    3-2578 5 NHCS NH HOOC--(CH.sub.2).sub.3 --                                    3-2579 5 CO NH MeSO.sub.2 NHCOCH(Me)                                          3-2580 5 NHCO NH MeSO.sub.2 NHCOCH(Me)                                        3-2581 5 NHCO -- MeSO.sub.2 NHCOCH(Me)                                        3-2582 5 NHCS NH MeSO.sub.2 NHCOCH(Me)                                        3-2583 5 -- NH HOOCCH.sub.2                                                   3-2584 5 -- NH MeOOCCH.sub.2                                                  3-2585 5 -- NH MeCH(COOH)                                                     3-2586 5 -- NH HOOC--(CH.sub.2).sub.2                                         3-2587 5 -- NH MeCH(COOMe)                                                    3-2588 5 -- NH HOOC--(CH.sub.2).sub.3 --                                      3-2589 5 NHCOCO -- OH                                                         3-2590 5 NHCOCO -- MeO                                                        3-2591 5 NHCOCO -- Eto                                                        3-2592 5 NHCOCO -- PrO                                                        3-2593 5 NHCOCO -- iPrO                                                       3-2594 5 NHCOCO -- BuO                                                        3-2595 5 NHCOCO -- iBuO                                                       3-2596 5 NHCOCO -- sBuO                                                       3-2597 5 NHCOCO -- sBuO                                                       3-2598 5 NHCOCO -- HxO                                                        3-2599 5 NHCOCO -- PhO                                                        3-2600 5 NHCOCO -- BnO                                                      3-2601                                                                              0     --             1,3-diox-IInd                                        3-2602 1 -- 1,3-diox-IInd                                                     3-2603 2 -- 1,3-diox-IInd                                                     3-2604 3 -- 1,3-diox-IInd                                                     3-2605 4 -- 1,3-diox-IInd                                                     3-2606 5 -- 1,3-diox-IInd                                                     3-2607 6 -- 1,3-diox-IInd                                                     3-2608 7 -- 1,3-diox-IInd                                                     3-2609 8 -- 1,3-diox-IInd                                                     3-2610 9 -- 1,3-diox-IInd                                                     3-2611 10 -- 1,3-diox-IInd                                                    3-2612 11 -- 1,3-diox-IInd                                                    3-2613 12 -- 1,3-diox-IInd                                                  3-2614                                                                              4     NHCONHSO.sub.2 NHCO                                                                          NH   Z-4                                             3-2615 4 NHCONHSO.sub.2 NHCO NH Pn                                            3-2616 2 O -- H                                                               3-2617 4 O -- H                                                               3-2618 5 O -- H                                                               3-2619 5 O -- Ph                                                              3-2620 5 O -- 2-Py                                                            3-2621 5 O -- 3-Py                                                            3-2622 5 O -- 4-Py                                                            3-2623 5 O -- Z-1                                                             3-2624 5 O -- Z-2                                                             3-2625 5 O -- Z-3                                                             3-2626 5 O -- Z-4                                                             3-2627 5 O -- Z-5                                                             3-2628 5 O -- Z-6                                                             3-2629 5 O -- Z-7                                                             3-2630 5 O -- Z-8                                                             3-2631 5 O -- Z-9                                                             3-2632 5 O -- Z-10                                                            3-2633 5 O -- Z-11                                                            3-2634 5 O -- Z-12                                                            3-2635 4 NHCO -- 3-Py                                                         3-2636 5 NHCO -- 3-Py                                                         3-2637 4 CO NH HOCH.sub.2 CH(CH.sub.3)CH.sub.2                                3-2638 5 CO NH HOCH.sub.2 CH(CH.sub.3)CH.sub.2                                3-2639 4 NHCO NH HOCH.sub.2 CH(CH.sub.3)CH.sub.2                              3-2640 5 NHCO NH HOCH.sub.2 CH(CH.sub.3)CH.sub.2                              3-2641 4 CO NH MeSO.sub.2 NHCOCH.sub.2                                        3-2642 5 CO NH MeSO.sub.2 NHCOCH.sub.2                                        3-2643 4 NHCO NH MeSO.sub.2 NHCOCH.sub.2                                      3-2644 5 NHCO NH MeSO.sub.2 NHCOCH.sub.2                                      3-2645 4 CO NH H.sub.2 NSO.sub.2 NHCOCH.sub.2                                 3-2646 5 CO NH H.sub.2 NSO.sub.2 NHCOCH.sub.2                                 3-2647 4 NHCO NH H.sub.2 NSO.sub.2 NHCOCH.sub.2                               3-2648 5 NHCO NH H.sub.2 NSO.sub.2 NHCOCH.sub.2                               3-2649 4 CO NH 1-(MeSO.sub.2 NHCO)-Et                                         3-2650 5 CO NH 1-(MeSO.sub.2 NHCO)-Et                                         3-2651 4 NHCO NH 1-(meSO.sub.2 NHCO)-Et                                       3-2652 5 NHCO NH 1-(MeSO.sub.2 NHCO)-Et                                       3-2653 4 CO NH 1-(H.sub.2 NSO.sub.2 NHCO)-Et                                  3-2654 5 CO NH 1-(H.sub.2 NSO.sub.2 NHCO)-Et                                  3-2655 4 NHCO NH 1-(H.sub.2 NSO.sub.2 NHCO)-Et                                3-2656 5 NHCO NH 1-(H.sub.2 NSO.sub.2 NHCO)-Et                                3-2657 4 CO NH HOOC--(CH.sub.2).sub.4                                         3-2658 5 CO NH HOOC--(CH.sub.2).sub.4                                         3-2659 4 NHCO NH HOOC--(CH.sub.2).sub.4                                       3-2660 5 NHCO NH HOOC--(CH.sub.2).sub.4                                       3-2661 4 CO NH HO--(CH.sub.2).sub.2                                           3-2662 5 CO NH HO--(CH.sub.2).sub.2                                           3-2663 4 NHCO NH HO--(CH.sub.2).sub.2                                         3-2664 5 NHCO NH HO--(CH.sub.2).sub.2                                         3-2665 4 CO NH HO--CH.sub.2 --CH(CH.sub.3)                                    3-2666 5 CO NH HO--CH.sub.2 --CH(CH.sub.3)                                    3-2667 4 NHCO NH HO--CH.sub.2 --CH(CH.sub.3)                                  3-2668 5 NHCO NH HO--CH.sub.2 --CH(CH.sub.3)                                  3-2669 4 CO NMe HOOC--(CH.sub.2).sub.3                                        3-2670 4 NHCO NMe HOOC--(CH.sub.2).sub.3                                      3-2671 5 NHCO NMe HOOC--(CH.sub.2).sub.3                                      3-2672 4 CONMeSO.sub.2 -- Me                                                  3-2673 5 CONMeSO.sub.2 -- Me                                                3-2674                                                                              4     CO             1-Indn                                               3-2675 5 CO 1-Indn                                                            3-2676 4 NHCO 1-Indn                                                          3-2677 5 NHCO 1-Indn                                                          3-2678 4 CO 2-(HOOC)-1-Indn                                                   3-2679 5 CO 2-(HOOC)-1-Indn                                                   3-2680 4 NHCO 2-(HOOC)-1-Indn                                                 3-2681 5 NHCO 2-(HOOC)-1-Indn                                                 3-2682 4 -- 2,4-diMe-2,5-diox-1-Imdd                                          3-2683 5 -- 3,4-diMe-2,5-diox-1-Imdd                                        ______________________________________                                    

Of the above compounds, preferred compounds are Compounds No.: 1-1, 1-2,1-3, 1-4, 1-5, 1-6, 1-7, 1-8, 1-9, 1-10, 1-11, 1-12, 1-13, 1-14, 1-15,1-16, 1-17, 1-18, 1-19, 1-20, 1-21, 1-22, 1-23, 1-24, 1-25, 1-26, 1-27,1-28, 1-29, 1-30, 1-31, 1-32, 1-33, 1-34, 1-35, 1-36, 1-37, 1-38, 1-39,1-40, 1-41, 1-42, 1-43, 1-44, 1-45, 1-46, 1-47, 1-48, 1-49, 1-50, 1-51,1-52, 1-53, 1-54, 1-55, 1-56, 1-57, 1-58, 1-59, 1-60, 1-61, 1-62, 1-63,1-64, 1-65, 1-66, 1-67, 1-68, 1-69, 1-70, 1-71, 1-72, 1-73, 1-74, 1-75,1-76, 1-77, 1-78, 1-79, 1-80, 1-81, 1-82, 1-232, 1-233, 1-234, 1-235,1-236, 1-237, 1-238, 1-239, 1-240, 1-241, 1-242, 1-243, 1-244, 1-245,1-246, 1-247, 1-248, 1-249, 1-250, 1-251, 1-252, 1-253, 1-254, 1-255,1-256, 1-257, 1-258, 1-259, 1-260, 1-261, 1-262, 1-263, 1-264, 1-265,1-266, 1-267, 1-268, 1-269, 1-270, 1-271, 1-272, 1-273, 1-274, 1-275,1-276, 1-277, 1-278, 1-279, 1-280, 1-281, 1-282, 1-283, 1-284, 1-285,1-286, 1-287, 1-288, 1-289, 1-290, 1-291, 1-292, 1-293, 1-294, 1-295,1-296, 1-297, 1-298, 1-299, 1-300, 1-301, 1-302, 1-303, 1-304, 1-305,1-306, 1-307, 1-308, 1-309, 1-310, 1-311, 1-312, 1-313, 1-314, 1-315,1-316, 1-317, 1-318, 1-319, 1-320, 1-321, 1-322, 1-323, 1-324, 1-325,1-326, 1-327, 1-328, 1-329, 1-330, 1-331, 1-332, 1-333, 1-334, 1-335,1-336, 1-337, 1-338, 1-339, 1-340, 1-341, 1-342, 1-343, 1-344, 1-345,1-346, 1-347, 1-348, 1-349, 1-350, 1-351, 1-352, 1-353, 1-354, 1-355,1-356, 1-357, 1-358, 1-359, 1-360, 1-361, 1-362, 1-363, 1-364, 1-365,1-366, 1-367, 1-368, 1-369, 1-370, 1-371, 1-372, 1-373, 1-374, 1-375,1-376, 1-377, 1-378, 1-379, 1-380, 1-381, 1-382, 1-383, 1-384, 1-385,1-386, 1-387, 1-388, 1-389, 1-390, 1-391, 1-392, 1-393, 1-394, 1-395,1-396, 1-397, 1-398, 1-399, 1-400, 1-401, 1-402, 1-403, 1-404, 1-405,1-406, 1-407, 1-408, 1-409, 1-410, 1-411, 1-412, 1-413, 1-414, 1-415,1-416, 1-417, 1-418, 1-419, 1-420, 1-421, 1-422, 1-423, 1-424, 1-425,1-426, 1-427, 1-428, 1-429, 1-430, 1-431, 1-432, 1-433, 1-434, 1-435,1-436, 1-437, 1-438, 1-439, 1-440, 1-441, 1-442, 1-443, 1-444, 1-445,1-446, 1-447, 1-448, 1-449, 1-450, 1-451, 1-452, 1-453, 1-454, 1-455,1-456, 1-457, 1-458, 1-459, 1-460, 1-461, 1-462, 1-463, 1-464, 1-465,1-466, 1-467, 1-468, 1-469, 1-470, 1-471, 1-472, 1-473, 1-474, 1-475,1-476, 1-477, 1-478, 1-479, 1-480, 1-481, 1-482, 1-483, 1-484, 1-485,1-486, 1-487, 1-488, 1-489, 1-490, 1-491, 1-492, 1-493, 1-494, 1-495,1-496, 1-497, 1-498, 1-499, 1-500, 1-501, 1-502, 1-503, 1-504, 1-505,1-506, 1-507, 1-508, 1-509, 1-510, 1-511, 1-512, 1-513, 1-514, 1-515,1-516, 1-517, 1-518, 1-519, 1-520, 1-521, 1-522, 1-523, 1-524, 1-525,1-526, 1-527, 1-528, 1-529, 1-530, 1-531, 1-532, 1-533, 1-534, 1-535,1-536, 1-537, 1-538, 1-539, 1-540, 1-541, 1-542, 1-543, 1-544, 1-545,1-546, 1-547, 1-548, 1-549, 1-550, 1-551, 1-552, 1-553, 1-554, 1-555,1-556, 1-557, 1-558, 1-559, 1-560, 1-561, 1-562, 1-563, 1-564, 1-565,1-566, 1-567, 1-568, 1-569, 1-570, 1-571, 1-572, 1-573, 1-574, 1-575,1-576, 1-577, 1-578, 1-579, 1-580, 1-581, 1-582, 1-583, 1-584, 1-585,1-586, 1-587, 1-588, 1-589, 1-590, 1-591, 1-592, 1-593, 1-594, 1-595,1-596, 1-597, 1-598, 1-599, 1-600, 1-601, 1-602, 1-603, 1-604, 1-605,1-606, 1-607, 1-608, 1-609, 1-610, 1-611, 1-612, 1-613, 1-614, 1-615,1-616, 1-617, 1-618, 1-619, 1-620, 1-621, 1-676, 1-677, 1-678, 1-679,1-680, 1-681, 1-682, 1-683, 1-684, 1-685, 1-686, 1-687, 1-688, 1-689,1-690, 1-691, 1-692, 1-693, 1-694, 1-695, 1-696, 1-697, 1-698, 1-699,1-700, 1-701, 1-702, 1-703, 1-704, 1-705, 1-706, 1-707, 1-708, 1-709,1-710, 1-711, 1-712, 1-713, 1-714, 1-715, 1-716, 1-717, 1-718, 1-719,1-720, 1-721, 1-722, 1-723, 1-724, 1-725, 1-726, 1-727, 1-728, 1-729,1-730, 1-731, 1-732, 1-733, 1-734, 1-735, 1-736, 1-737, 1-738, 1-739,1-740, 1-741, 1-742, 1-743, 1-744, 1-745, 1-746, 1-747, 1-748, 1-749,1-750, 1-751, 1-752, 1-753, 1-754, 1-755, 1-756, 1-757, 1-758, 1-759,1-760, 1-761, 1-762, 1-763, 1-764, 1-765, 1-766, 1-767, 1-768, 1-769,1-770, 1-771, 1-772, 1-773, 1-774, 1-775, 1-776, 1-777, 1-778, 1-779,1-780, 1-781, 1-782, 1-783, 1-784, 1-785, 1-786, 1-787, 1-788, 1-789,1-790, 1-791, 1-792, 1-793, 1-794, 1-795, 1-796, 1-797, 1-798, 1-799,1-800, 1-801, 1-802, 1-803, 1-804, 1-805, 1-806, 1-807, 1-808, 1-809,1-810, 1-811, 1-812, 1-813, 1-814, 1-815, 1-816, 1-817, 1-818, 1-819,1-820, 1-821, 1-822, 1-823, 1-824, 1-825, 1-826, 1-827, 1-828, 1-829,1-830, 1-831, 1-832, 1-833, 1-834, 1-835, 1-836, 1-837, 1-838, 1-839,1-840, 1-841, 1-842, 1-843, 1-844, 1-845, 1-846, 1-847, 1-848, 1-849,1-850, 1-851, 1-852, 1-853, 1-854, 1-855, 1-856, 1-857, 1-858, 1-859,1-860, 1-861, 1-862, 1-863, 1-1112, 1-1113, 1-1114, 1-1115, 1-1116,1-1117, 1-1118, 1-1119, 1-1120, 1-1121, 1-1122, 1-1123, 1-1124, 1-1125,1-1126, 1-1127, 1-1128, 1-1129, 1-1130, 1-1131, 1-1132, 1-1133, 1-1134,1-1135, 1-1136, 1-1137, 1-1138, 1-1139, 1-1140, 1-1141, 1-1142, 1-1143,1-1144, 1-1145, 1-1146, 1-1147, 1-1148, 1-1149, 1-1150, 1-1151, 1-1152,1-1153, 1-1154, 1-1155, 1-1156, 1-1157, 1-1158, 1-1159, 1-1160, 1-1161,1-1162, 1-1163, 1-1164, 1-1165, 1-1166, 1-1167, 1-1168, 1-1169, 1-1224,1-1258, 1-1259, 1-1260, 1-1261, 1-1262, 1-1263, 1-1264, 1-1265, 1-1266,1-1267, 1-1268, 1-1269, 1-1270, 1-1271, 1-1272, 1-1273, 1-1274, 1-1275,1-1276, 1-1277, 1-1278, 1-1279, 1-1280, 1-1281, 1-1282, 1-1283, 1-1284,1-1285, 1-1286, 1-1287, 1-1288, 1-1289, 1-1290, 1-1291, 1-1292, 1-1293,1-1294, 1-1295, 1-1296, 1-1297, 1-1298, 1-1299, 1-1300, 1-1301, 1-1302,1-1303, 1-1304, 1-1305, 1-1306, 1-1307, 1-1308, 1-1309, 1-1310, 1-1311,1-1312, 1-1313, 1-1314, 1-1315, 1-1316, 1-1317, 1-1318, 1-1319, 1-1320,1-1321, 1-1322, 1-1323, 1-1324, 1-1325, 1-1326, 1-1327, 1-1328, 1-1329,1-1330, 1-1331, 1-1332, 1-1333, 1-1334, 1-1335, 1-1336, 1-1337, 1-1338,1-1339, 1-1340, 1-1341, 1-1342, 1-1343, 1-1344, 1-1345, 1-1346, 1-1347,1-1348, 1-1349, 1-1350, 1-1351, 1-1352, 1-1353, 1-1354, 1-1355, 1-1356,1-1357, 1-1358, 1-1359, 1-1360, 1-1361, 1-1362, 1-1363, 1-1364, 1-1365,1-1366, 1-1367, 1-1368, 1-1369, 1-1370, 1-1371, 1-1372, 1-1373, 1-1374,1-1375, 1-1376, 1-1377, 1-1378, 1-1379, 1-1380, 1-1381, 1-1382, 1-1383,1-1532, 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3-402,3-403, 3-404, 3-405, 3-406, 3-407, 3-408, 3-409, 3-410, 3-411, 3-412,3-413, 3-414, 3-415, 3-416, 3-417, 3-418, 3-419, 3-420, 3-421, 3-422,3-423, 3-424, 3-425, 3-426, 3-427, 3-428, 3-429, 3-430, 3-431, 3-432,3-433, 3-434, 3-435, 3-436, 3-437, 3-438, 3-439, 3-440, 3-441, 3-442,3-443, 3-444, 3-445, 3-446, 3-447, 3-448, 3-449, 3-450, 3-451, 3-452,3-453, 3-454, 3-455, 3-456, 3-457, 3-458, 3-459, 3-460, 3-461, 3-462,3-463, 3-464, 3-465, 3-466, 3-467, 3-468, 3-469, 3-470, 3-471, 3-472,3-473, 3-474, 3-475, 3-476, 3-477, 3-478, 3-479, 3-480, 3-481, 3-482,3-483, 3-484, 3-485, 3-486, 3-487, 3-488, 3-489, 3-490, 3-491, 3-492,3-493, 3-494, 3-495, 3-496, 3-497, 3-498, 3-499, 3-500, 3-501, 3-502,3-503, 3-504, 3-505, 3-506, 3-507, 3-508, 3-509, 3-510, 3-511, 3-512,3-513, 3-514, 3-515, 3-516, 3-517, 3-518, 3-519, 3-520, 3-521, 3-522,3-523, 3-524, 3-525, 3-526, 3-527, 3-528, 3-529, 3-530, 3-531, 3-532,3-533, 3-534, 3-535, 3-536, 3-537, 3-538, 3-539, 3-540, 3-541, 3-542,3-543, 3-544, 3-545, 3-546, 3-547, 3-548, 3-549, 3-550, 3-551, 3-552,3-553, 3-554, 3-555, 3-556, 3-557, 3-558, 3-559, 3-560, 3-561, 3-562,3-563, 3-564, 3-565, 3-566, 3-567, 3-568, 3-569, 3-570, 3-571, 3-572,3-573, 3-574, 3-575, 3-576, 3-577, 3-578, 3-579, 3-580, 3-581, 3-582,3-583, 3-584, 3-585, 3-586, 3-587, 3-588, 3-589, 3-590, 3-591, 3-592,3-593, 3-594, 3-595, 3-596, 3-597, 3-598, 3-599, 3-600, 3-601, 3-602,3-603, 3-604, 3-605, 3-606, 3-607, 3-608, 3-609, 3-610, 3-611, 3-612,3-613, 3-614, 3-615, 3-616, 3-617, 3-618, 3-619, 3-620, 3-621, 3-676,3-677, 3-678, 3-679, 3-680, 3-681, 3-682, 3-683, 3-684, 3-685, 3-686,3-687, 3-688, 3-689, 3-690, 3-691, 3-692, 3-693, 3-694, 3-695, 3-696,3-697, 3-698, 3-699, 3-700, 3-701, 3-702, 3-703, 3-704, 3-705, 3-706,3-707, 3-708, 3-709, 3-710, 3-711, 3-712, 3-713, 3-714, 3-715, 3-716,3-717, 3-718, 3-719, 3-720, 3-721, 3-722, 3-723, 3-724, 3-725, 3-726,3-727, 3-728, 3-729, 3-730, 3-731, 3-732, 3-733, 3-734, 3-735, 3-736,3-737, 3-738, 3-739, 3-740, 3-741, 3-742, 3-743, 3-744, 3-745, 3-746,3-747, 3-748, 3-749, 3-750, 3-751, 3-752, 3-753, 3-754, 3-755, 3-756,3-757, 3-758, 3-759, 3-760, 3-761, 3-762, 3-763, 3-764, 3-765, 3-766,3-767, 3-768, 3-769, 3-770, 3-771, 3-772, 3-773, 3-774, 3-775, 3-776,3-777, 3-778, 3-779, 3-780, 3-781, 3-782, 3-783, 3-784, 3-785, 3-786,3-787, 3-788, 3-789, 3-790, 3-791, 3-792, 3-793, 3-794, 3-795, 3-796,3-797, 3-798, 3-799, 3-800, 3-801, 3-802, 3-803, 3-804, 3-805, 3-806,3-807, 3-808, 3-809, 3-810, 3-811, 3-812, 3-813, 3-814, 3-815, 3-816,3-817, 3-818, 3-819, 3-820, 3-821, 3-822, 3-823, 3-824, 3-825, 3-826,3-827, 3-828, 3-829, 3-830, 3-831, 3-832, 3-833, 3-834, 3-835, 3-836,3-837, 3-838, 3-839, 3-840, 3-841, 3-842, 3-843, 3-844, 3-845, 3-846,3-847, 3-848, 3-849, 3-850, 3-851, 3-852, 3-853, 3-854, 3-855, 3-856,3-857, 3-858, 3-859, 3-860, 3-861, 3-862, 3-863, 3-1112, 3-1113, 3-1114,3-1115, 3-1116, 3-1117, 3-1118, 3-1119, 3-1120, 3-1121, 3-1122, 3-1123,3-1124, 3-1125, 3-1126, 3-1127, 3-1128, 3-1129, 3-1130, 3-1131, 3-1132,3-1133, 3-1134, 3-1135, 3-1136, 3-1137, 3-1138, 3-1139, 3-1140, 3-1141,3-1142, 3-1143, 3-1144, 3-1145, 3-1146, 3-1147, 3-1148, 3-1149, 3-1150,3-1151, 3-1152, 3-1153, 3-1154, 3-1155, 3-1156, 3-1157, 3-1158, 3-1159,3-1160, 3-1161, 3-1162, 3-1163, 3-1164, 3-1165, 3-1166, 3-1167, 3-1168,3-1169, 3-1224, 3-1258, 3-1259, 3-1260, 3-1261, 3-1262, 3-1263, 3-1264,3-1265, 3-1266, 3-1267, 3-1268, 3-1269, 3-1270, 3-1271, 3-1272, 3-1273,3-1274, 3-1275, 3-1276, 3-1277, 3-1278, 3-1279, 3-1280, 3-1281, 3-1282,3-1283, 3-1284, 3-1285, 3-1286, 3-1287, 3-1288, 3-1289, 3-1290, 3-1291,2-1292, 3-1293, 3-1294, 3-1295, 3-1296, 3-1297, 3-1298, 3-1299, 3-1300,3-1301, 3-1302, 3-1303, 3-1304, 3-1305, 3-1306 3-1307, 3-1308, 3-1309,3-1310, 3-1311, 3-1312, 3-1313, 3-1314, 3-1315, 3-1316, 3-1317, 3-1318,3-1319, 3-1320, 3-1321, 3-1322, 3-1323, 3-1324, 3-1325, 3-1326, 3-1327,3-1328, 3-1329, 3-1330, 3-1331, 3-1332, 3-1333, 3-1334, 3-1335, 3-1336,3-1337, 3-1338, 3-1339, 3-1340, 3-1341, 3-1342, 3-1343, 3-1344, 3-1345,3-1346, 3-1347, 3-1348, 3-1349, 3-1350, 3-1351, 3-1352, 3-1353, 3-1354,3-1355, 3-1356, 3-1357, 3-1358, 3-1359, 3-1360, 3-1361, 3-1362, 3-1363,3-1364, 3-1365, 3-1366, 3-1367, 3-1368, 3-1369, 3-1370, 3-1371, 3-1372,3-1373, 3-1374, 3-1375, 3-1376, 3-1377, 3-1378, 3-1379, 3-1380, 3-1381,3-1382, 3-1383, 3-1532, 3-1533, 3-1534, 3-1535, 3-1536, 3-1537, 3-1538,3-1539, 3-1540, 3-1541, 3-1542, 3-1543, 3-1544, 3-1545, 3-1546, 3-1547,3-1548, 3-1549, 3-1550, 3-1551, 3-1552, 3-1553, 3-1554, 3-1555, 3-1556,3-1557, 3-1558, 3-1559, 3-1560, 3-1561, 3-1562, 3-1563, 3-1564, 3-1565,3-1566, 3-1567, 3-1568, 3-1569, 3-1570, 3-1571, 3-1572, 3-1573, 3-1574,3-1575, 3-1576, 3-1577, 3-1578, 3-1579, 3-1580, 3-1581, 3-1582, 3-1583,3-1584, 3-1585, 3-1586, 3-1587, 3-1588, 3-1589, 3-1590, 3-1591, 3-1592,3-1593, 3-1594, 3-1595, 3-1596, 3-1597, 3-1598, 3-1600, 3-1601, 3-1601,3-1602, 3-1603, 3-1604, 3-1605, 3-1606, 3-1607, 3-1608, 3-1609, 3-1610,3-1611, 3-1612, 3-1613, 3-1614 3-1615, 3-1616, 3-1617, 3-1618, 3-1619,3-1620, 3-1621, 3-1622, 3-1623, 3-1624, 3-1625, 3-1626, 3-1627, 3-1628,3-1629, 3-1630, 3-1631, 3-1632, 3-1633, 3-1634, 3-1635, 3-1636, 3-1637,3-1638, 3-1639, 3-1640, 3-1641, 3-1642, 3-1643, 3-1644, 3-1645, 3-1646,3-1647, 3-1648, 3-1649, 3-1650, 3-1651, 3-1652, 3-1653, 3-1654, 3-1655,3-1656, 3-1657, 3-1658, 3-1659, 3-1660, 3-1661, 3-1662, 3-1663, 3-1664,3-1665, 3-1666, 3-1667, 3-1668, 3-1669, 3-1670, 3-1671, 3-1672, 3-1673,3-1674, 3-1675, 3-1676, 3-1677, 3-1678, 3-1679, 3-1680, 3-1681, 3-1682,3-1683, 3-1684, 3-1685, 3-1686, 3-1687, 3-1688, 3-1689, 3-1690, 3-1691,3-1692, 3-1693, 3-1694, 3-1695, 3-1696, 3-1697, 3-1698, 3-1699, 3-1700,3-1701, 3-1702, 3-1703, 3-1704, 3-1705, 3-1706, 3-1707, 3-1708, 3-1709,3-1710, 3-1711, 3-1712, 3-1713, 3-1714, 3-1715, 3-1716, 3-1717, 3-1718,3-1719, 3-1720, 3-1721, 3-1722, 3-1723, 3-1724, 3-1725, 3-1726, 3-1727,3-1728, 3-1729, 3-1730, 3-1731, 3-1732, 3-1733, 3-1734, 3-1735, 3-1736,3-1737, 3-1738, 3-1739, 3-1740, 3-1741, 3-1742, 3-1743, 3-1744, 3-1745,3-1746, 3-1747, 3-1748, 3-1749, 3-1750, 3-1751, 3-1752, 3-1753, 3-1754,3-1755, 3-1756, 3-1757, 3-1758, 3-1759, 3-1760, 3-1761, 3-1762, 3-1763,3-1764, 3-1765, 3-1766, 3-1767, 3-1768, 3-1769, 3-1770, 3-1771, 3-1772,3-1773, 3-1774, 3-1775, 3-1776, 3-1777, 3-1778, 3-1779, 3-1780, 3-1781,3-1782, 3-1783, 3-1784, 3-1785, 3-1786, 3-1787, 3-1788, 3-1789, 3-1790,3-1791, 3-1792, 3-1793, 3-1794, 3-1795, 3-1796, 3-1797, 3-1798, 3-1799,3-1800, 3-1801, 3-1802, 3-1803, 3-1804, 3-1805, 3-1806, 3-1807, 3-1808,3-1809, 3-1810, 3-1811, 3-1812, 3-1813, 3-1814, 3-1815, 3-1816, 3-1817,3-1818, 3-1819, 3-1820, 3-1821, 3-1822, 3-1823, 3-1824, 3-1825, 3-1826,3-1827, 3-1828, 3-1829, 3-1830, 3-1831, 3-1832, 3-1833, 3-1834, 3-1835,3-1836, 3-1837, 3-1838, 3-1839, 3-1840, 3-1841, 3-1842, 3-1843, 3-1844,3-1845, 3-1846, 3-1847, 3-1848, 3-1849, 3-1850, 3-1851, 3-1852, 3-1853,3-1854, 3-1855, 3-1856, 3-1857, 3-1858, 3-1859, 3-1860, 3-1861, 3-1862,3-1863, 3-1864, 3-1865, 3-1866, 3-1867, 3-1868, 3-1869, 3-1870, 3-1871,3-1872, 3-1873, 3-1874, 3-1875, 3-1876, 3-1877, 3-1878, 3-1879, 3-1880,3-1881, 3-1882, 3-1883, 3-1884, 3-1885, 3-1886, 3-1887, 3-1888, 3-1889,3-1890, 3-1891, 3-1892, 3-1893, 3-1894, 3-1895, 3-1896, 3-1897, 3-1898,3-1899, 3-1900, 3-1901, 3-1902, 3-1903, 3-1904, 3-1905, 3-1906, 3-1907,3-1908, 3-1909, 3-1910, 3-1911, 3-1912, 3-1913, 3-1914, 3-1915, 3-1916,3-1917, 3-1918, 3-1919, 3-1920, 3-1921, 3-1962, 3-1963, 3-1964, 3-1965,3-1966, 3-1967, 3-1968, 3-1969, 3-1970, 3-1971, 3-1972, 3-1973, 3-1974,3-1975, 3-1976, 3-1977, 3-1978, 3-1979, 3-1980, 3-1981, 3-1982, 3-1983,3-1984, 3-1985, 3-1986, 3-1987, 3-1988, 3-1989, 3-1990, 3-1991, 3-1992,3-1993, 3-1994, 3-1995, 3-1996, 3-1997, 3-1998, 3-1999, 3-2000, 3-2001,3-2002, 3-2003, 3-2004, 3-2005, 3-2006, 3-2007, 3-2008, 3-2009, 3-2010,3-2011, 3-2012, 3-2013, 3-2014, 3-2015, 3-2016, 3-2017, 3-2018, 3-2019,3-2020, 3-2021, 3-2022, 3-2023, 3-2024, 3-2025, 3-2026, 3-2027, 3-2028,3-2029, 3-2030, 3-2031, 3-2032, 3-2033, 3-2034, 3-2035, 3-2036, 3-2037,3-2038, 3-2039, 3-2040, 3-2041, 3-2042, 3-2043, 3-2044, 3-2045, 3-2046,3-2047, 3-2048, 3-2049, 3-2050, 3-2051, 3-2052, 3-2053, 3-2054, 3-2055,3-2056, 3-2057, 3-2058, 3-2059, 3-2060, 3-2061, 3-2062, 3-2063, 3-2064,3-2065, 3-2066, 3-2067, 3-2068, 3-2069, 3-2070, 3-2071, 3-2072, 3-2073,3-2074, 3-2075, 3-2076, 3-2077, 3-2078, 3-2079, 3-2080, 3-2081, 3-2082,3-2083, 3-2084, 3-2085, 3-2086, 3-2087, 3-2088, 3-2089, 3-2090, 3-2091,3-2092, 3-2093, 3-2094, 3-2095, 3-2096, 3-2097, 3-2098, 3-2099, 3-2100,3-2101, 3-2102, 3-2103, 3-2104, 3-2105, 3-2106, 3-2107, 3-2108, 3-2109,3-2110, 3-2111, 3-2112, 3-2113, 3-2114, 3-2115, 3-2116, 3-2117, 3-2118,3-2119, 3-2120, 3-2121, 3-2122, 3-2123, 3-2124, 3-2125, 3-2126, 3-2127,3-2128, 3-2129, 3-2130, 3-2131, 3-2132, 3-2133, 3-2134, 3-2135, 3-2136,3-2137, 3-2138, 3-2139, 3-2140, 3-2141, 3-2142, 3-2143, 3-2144, 3-2145,3-2146, 3-2147, 3-2148, 3-2149, 3-2150, 3-2151, 3-2152, 3-2153, 3-2154,3-2155, 3-2156, 3-2157, 3-2158, 3-2159, 3-2160, 3-2161, 3-2162, 3-2163,3-2429, 3-2430, 3-2431, 3-2432, 3-2433, 3-2434, 3-2435, 3-2436, 3-2437,3-2438, 3-2439, 3-2440, 3-2441, 3-2442, 3-2443, 3-2444, 3-2445, 3-2446,3-2447, 3-2448, 3-2449, 3-2450, 3-2451, 3-2452, 3-2453, 3-2454, 3-2455,3-2456, 3-2457, 3-2458, 3-2459, 3-2460, 3-2461, 3-2462, 3-2463, 3-2464,3-2465, 3-2466, 3-2467, 3-2468, 3-2469, 3-2470, 3-2471, 3-2472, 3-2473,3-2474, 3-2475, 3-2476, 3-2477, 3-2478, 3-2479, 3-2480, 3-2481, 3-2482,3-2483, 3-2484, 3-2485, 3-2486, 3-2487, 3-2488, 3-2489, 3-2490, 3-2491,3-2492, 3-2493, 3-2494, 3-2495, 3-2496, 3-2497, 3-2498, 3-2499, 3-2500,3-2501, 3-2502, 3-2503, 3-2504, 3-2505, 3-2506, 3-2507, 3-2508, 3-2509,3-2510, 3-2511, 3-2512, 3-2513, 3-2514, 3-2515, 3-2516, 3-2517, 3-2518,3-2519, 3-2520, 3-2521, 3-2522, 3-2523, 3-2524, 3-2525, 3-2526, 3-2527,3-2528, 3-2529, 3-2530, 3-2531, 3-2532, 3-2533, 3-2534, 3-2535, 3-2536,3-2537, 3-2538, 3-2539, 3-2540, 3-2541, 3-2542, 3-2543, 3-2544, 3-2545,3-2546, 3-2547, 3-2548, 3-2549, 3-2550, 3-2551, 3-2552, 3-2553, 3-2554,3-2555, 3-2556, 3-2557, 3-2558, 3-2559, 3-2560, 3-2561, 3-2562, 3-2563,3-2564, 3-2565, 3-2566, 3-2567, 3-2568, 3-2569, 3-2570, 3-2571, 3-2572,3-2573, 3-2574, 3-2575, 3-2576, 3-2577, 3-2578, 3-2579, 3-2580, 3-2581,3-2582, 3-2583, 3-2584, 3-2585, 3-2586, 3-2587, 3-2588, 3-2589, 3-2590,3-2591, 3-2592, 3-2593, 3-2594, 3-2595, 3-2596, 3-2597, 3-2598, 3-2599,3-2600, 3-2601, 3-2602, 3-2603, 3-2604, 3-2605, 3-2606, 3-2607, 3-2608,3-2609, 3-2610, 3-2611, 3-2612, 3-2613, 3-2614, 3-2657, 3-2665, 3-2667,and 3-2669.

The following compounds are more preferred, that is Compounds No.: 1-2,1-3, 1-4, 1-5, 1-6, 1-7, 1-8, 1-9, 1-10, 1-11, 1-12, 1-13, 1-14, 1-15,1-16, 1-17, 1-18, 1-19, 1-20, 1-21, 1-22, 1-23, 1-24, 1-25, 1-26, 1-27,1-28, 1-29, 1-30, 1-31, 1-32, 1-33, 1-34, 1-35, 1-36, 1-37, 1-38, 1-39,1-40, 1-41, 1-42, 1-43, 1-44, 1-45, 1-46, 1-47, 1-48, 1-49, 1-50, 1-51,1-52, 1-53, 1-54, 1-55, 1-56, 1-57, 1-58, 1-59, 1-60, 1-61, 1-62, 1-63,1-64, 1-65, 1-66, 1-67, 1-68, 1-69, 1-70, 1-71, 1-72, 1-73, 1-74, 1-75,1-76, 1-77, 1-78, 1-79, 1-80, 1-271, 1-272, 1-273, 1-274, 1-275, 1-276,1-277, 1-278, 1-279, 1-279, 1-280, 1-281, 1-282, 1-283, 1-284, 1-285,1-286, 1-287, 1-288, 1-289, 1-290, 1-291, 1-292, 1-293, 1-294, 1-295,1-296, 1-297, 1-298, 1-299, 1-300, 1-301, 1-302, 1-303, 1-304, 1-305,1-306, 1-307, 1-308, 1-309, 1-310, 1-311, 1-312, 1-313, 3-314, 1-315,1-316, 1-317, 1-318, 1-319, 1-320, 1-321, 1-322, 1-323, 1-324, 1-325,1-326, 1-327, 1-328, 1-329, 1-330, 1-331, 1-332, 1-333, 1-334, 1-335,1-336, 1-337, 1-338, 1-339, 1-340, 1-341, 1-342, 1-343, 1-344, 1-345,1-346, 1-347, 1-348, 1-349, 1-350, 1-351, 1-352, 1-353, 1-354, 1-355,1-356, 1-357, 1-358, 1-359, 1-360, 1-361, 1-362, 1-363, 1-364, 1-365,1-366, 1-367, 1-368, 1-369, 1-370, 1-371, 1-372, 1-373, 1-374, 1-375,1-376, 1-377, 1-378, 1-379, 1-380, 1-381, 1-382, 1-383, 1-384, 1-385,1-386, 1-387, 1-388, 1-389, 1-390, 1-391, 1-392, 1-393, 1-394, 1-395,1-396, 1-397, 1-398, 1-399, 1-400, 1-401, 1-402, 1-403, 1-404, 1-405,1-406, 1-407, 1-408, 1-409, 1-410, 1-411, 1-412, 1-413, 1-414, 1-415,1-416, 1-417, 1-418, 1-419, 1-420, 1-421, 1-422, 1-423, 1-424, 1-425,1-426, 1-427, 1-428, 1-429, 1-430, 1-431, 1-432, 1-433, 1-434, 1-435,1-436, 1-437, 1-438, 1-439, 1-440, 1-441, 1-442, 1-443, 1-444, 1-445,1-446, 1-447, 1-448, 1-449, 1-450, 1-451, 1-452, 1-453, 1-454, 1-455,1-456, 1-457, 1-458, 1-459, 1-460, 1-461, 1-462, 1-463, 1-464, 1-465,1-466, 1-467, 1-468, 1-469, 1-470, 1-471, 1-472, 1-473, 1-474, 1-475,1-476, 1-477, 1-478, 1-479, 1-480, 1-481, 1-482, 1-483, 1-484, 1-485,1-486, 1-487, 1-488, 1-489, 1-490, 1-491, 1-492, 1-493, 1-494, 1-495,1-496, 1-497, 1-498, 1-499, 1-500, 1-501, 1-502, 1-503, 1-504, 1-505,1-506, 1-507, 1-508, 1-509, 1-510, 1-511, 1-512, 1-513, 1-514, 1-515,1-516, 1-517, 1-518, 1-519, 1-520, 1-521, 1-522, 1-523, 1-524, 1-525,1-526, 1-527, 1-528, 1-529, 1-530, 1-531, 1-532, 1-533, 1-534, 1-535,1-536, 1-537, 1-538, 1-539, 1-676, 1-677, 1-678, 1-679, 1-680, 1-681,1-682, 1-683, 1-684, 1-685, 1-686, 1-687, 1-688, 1-689, 1-690, 1-691,1-692, 1-693, 1-694, 1-695, 1-696, 1-697, 1-698, 1-699, 1-700, 1-701,1-702, 1-703, 1-704, 1-705, 1-706, 1-707, 1-708, 1-709, 1-710, 1-711,1-712, 1-713, 1-714, 1-715, 1-716, 1-717, 1-718, 1-719, 1-720, 1-721,1-722, 1-723, 1-724, 1-725, 1-726, 1-727, 1-728, 1-729, 1-730, 1-731,1-732, 1-733, 1-734, 1-735, 1-736, 1-737, 1-738, 1-739, 1-740, 1-741,1-742, 1-743, 1-744, 1-745, 1-746, 1-747, 1-748, 1-749, 1-750, 1-751,1-752, 1-753, 1-754, 1-755, 1-756, 1-757, 1-758, 1-759, 1-760, 1-761,1-762, 1-763, 1-764, 1-765, 1-766, 1-767, 1-768, 1-769, 1-770, 1-771,1-772, 1-773, 1-774, 1-775, 1-776, 1-777, 1-778, 1-779, 1-780, 1-781,1-782, 1-783, 1-784, 1-785, 1-786, 1-787, 1-788, 1-789, 1-790, 1-791,1-792, 1-793, 1-794, 1-795, 1-796, 1-797, 1-798, 1-799, 1-800, 1-801,1-802, 1-803, 1-804, 1-805, 1-806, 1-807, 1-808, 1-809, 1-810, 1-811,1-812, 1-813, 1-814, 1-815, 1-816, 1-817, 1-818, 1-819, 1-820, 1-821,1-822, 1-823, 1-824, 1-825, 1-826, 1-827, 1-828, 1-829, 1-830, 1-831,1-832, 1-833, 1-834, 1-835, 1-836, 1-837, 1-838, 1-839, 1-840, 1-841,1-842, 1-843, 1-844, 1-845, 1-846, 1-847, 1-848, 1-849, 1-850, 1-851,1-852, 1-853, 1-854, 1-855, 1-856, 1-857, 1-858, 1-859, 1-860, 1-861,1-862, 1-863, 1-1112, 1-1113, 1-1114, 1-1115, 1-1116, 1-1117, 1-1118,1-1119, 1-1120, 1-1121, 1-1122, 1-1123, 1-1124, 1-1125, 1-1126, 1-1127,1-1128, 1-1129, 1-1130, 1-1131, 1-1132, 1-1133, 1-1134, 1-1135, 1-1136,1-1137, 1-1138, 1-1139, 1-1140, 1-1141, 1-1142, 1-1143, 1-1144, 1-1145,1-1146, 1-1147, 1-1148, 1-1224, 1-1258, 1-1259, 1-1260, 1-1261, 1-1262,1-1263, 1-1264, 1-1265, 1-1266, 1-1267, 1-1268, 1-1269, 1-1270, 1-1271,1-1272, 1-1273, 1-1274, 1-1275, 1-1276, 1-1277, 1-1278, 1-1279, 1-1280,1-1962, 1-1963, 1-1964, 1-1965, 1-1966, 1-1967, 1-1968, 1-1969, 1-1970,1-1971, 1-1972, 1-1973, 1-1974, 1-1975, 1-1976, 1-1977, 1-1978, 1-1979,1-1980, 1-1981, 1-1982, 1-1983, 1-1984, 1-1985, 1-1986, 1-1987, 1-1988,1-1989, 1-1990, 1-1991, 1-1992, 1-1993, 1-2470, 1-2471, 1-2472, 1-2473,1-2474, 1-2475, 1-2476, 1-2477, 1-2478, 1-2479, 1-2480, 1-2481, 1-2482,1-2483, 1-2484, 1-2485, 1-2486, 1-2487, 1-2488, 1-2489, 1-2490, 1-2491,1-2492, 1-2493, 1-2494, 1-2495, 1-2496, 1-2497, 1-2498, 1-2499, 1-2500,1-2501, 1-2502, 1-2503, 1-2504, 1-2505, 1-2506, 1-2507, 1-2508, 1-2509,1-2510, 1-2511, 1-2512, 1-2513, 1-2514, 1-2515, 1-2516, 1-2517, 1-2518,1-2519, 1-2520, 1-2521, 1-2522, 1-2523, 1-2524, 1-2525, 1-2526, 1-2527,1-2528, 1-2529, 1-2530, 1-2531, 1-2532, 1-2533, 1-2534, 1-2535, 1-2536,1-2537, 1-2538, 1-2539, 1-2540, 1-2541, 1-2542, 1-2543, 1-2544, 1-2545,1-2546, 1-2547, 1-2548, 1-2549, 1-2550, 1-2551, 1-2552, 1-2553, 1-2554,1-2555, 1-2556, 1-2557, 1-2558, 1-2559, 1-2660, 1-2661, 1-2662, 1-2663,1-2664, 1-2565, 1-2566, 1-2567, 1-2568, 1-2569, 1-2570, 1-2571, 1-2572,1-2573, 1-2574, 1-2575, 1-2576, 1-2577, 1-2578, 1-2579, 1-2580, 1-2581,1-2582, 1-2583, 1-2584, 1-2585, 1-2586, 1-2587, 1-2588, 1-2589, 1-2590,1-2591, 1-2592, 1-2593, 1-2594, 1-2595, 1-2596, 1-2597, 1-2598, 1-2599,1-2600, 1-2601, 1-2602, 1-2603, 1-2604, 1-2605, 1-2606, 1-2607, 1-2608,1-2609, 1-2610, 1-2611, 1-2612, 1-2613, 1-2614, 1-2657, 1-2665, 1-2667and 1-2669.

The following compounds are still more preferred, that is Compounds No.:1-41, 1-42, 1-43, 1-44, 1-45, 1-46, 1-47, 1-48, 1-49, 1-50, 1-51, 1-52,1-53, 1-54, 1-55, 1-56, 1-57, 1-58, 1-59, 1-60, 1-61, 1-62, 1-63, 1-64,1-65, 1-66, 1-67, 1-68, 1-69, 1-70, 1-71, 1-72, 1-73, 1-74, 1-75, 1-76,1-77, 1-78, 1-79, 1-80, 1-271, 1-272, 1-273, 1-274, 1-275, 1-276, 1-277,1-278, 1-279, 1-280, 1-281, 1-282, 1-283, 1-284, 1-285, 1-286, 1-457,1-458, 1-459, 1-460, 1-461, 1-462, 1-463, 1-464, 1-465, 1-466, 1-467,1-468, 1-469, 1-470, 1-471, 1-472, 1-473, 1-474, 1-475, 1-476, 1-477,1-478, 1-479, 1-480, 1-481, 1-482, 1-483, 1-484, 1-485, 1-486, 1-487,1-488, 1-489, 1-490, 1-491, 1-492, 1-493, 1-494, 1-495, 1-496, 1-497,1-498, 1-499, 1-500, 1-501, 1-502, 1-503, 1-504, 1-505, 1-506, 1-507,1-508, 1-509, 1-510, 1-511, 1-512, 1-513, 1-514, 1-515, 1-516, 1-517,1-518, 1-519, 1-520, 1-521, 1-522, 1-523, 1-524, 1-525, 1-526, 1-527,1-528, 1-529, 1-530, 1-531, 1-532, 1-533, 1-534, 1-535, 1-536, 1-537,1-538, 1-539, 1-733, 1-734, 1-735, 1-736, 1-737, 1-738, 1-739, 1-740,1-741, 1-742, 1-743, 1-744, 1-745, 1-746, 1-747, 1-748, 1-749, 1-750,1-815, 1-816, 1-817, 1-818, 1-819, 1-820, 1-821, 1-822, 1-824, 1-824,1-825, 1-826, 1-827, 1-828, 1-829, 1-830, 1-831, 1-832, 1-833, 1-834,1-835, 1-836, 1-837, 1-838, 1-839, 1-840, 1-841, 1-842, 1-843, 1-844,1-845, 1-846, 1-847, 1-848, 1-849, 1-850, 1-851, 1-852, 1-853, 1-854,1-855, 1-856, 1-857, 1-858, 1-859, 1-860, 1-861, 1-862, 1-863, 1-1129,1-1130, 1-1131, 1-1132, 1-1133, 1-1134, 1-1135, 1-1136, 1-1137, 1-1138,1-1139, 1-1140, 1-1141, 1-1142, 1-1143, 1-1144, 1-1145, 1-1146, 1-1147,1-1148, 1-1224, 1-1258, 1-1259, 1-1260, 1-1261, 1-1262, 1-1263, 1-1264,1-1265, 1-1266, 1-1267, 1-1268, 1-1269, 1-1270, 1-1271, 1-1272, 1-1273,1-1274, 1-1275, 1-1276, 1-1277, 1-1278, 1-1279, 1-1280, 1-1962, 1-1963,1-1964, 1-1965, 1-1966, 1-1967, 1-1968, 1-1969, 1-1970, 1-1971, 1-1972,1-1973, 1-1974, 1-1975, 1-1976, 1-1977, 1-1978, 1-1979, 1-1980, 1-1981,1-1982, 1-1983, 1-1984, 1-1985, 1-1986, 1-1987, 1-1988, 1-1989, 1-1990,1-1991, 1-1992, 1-1993, 1-2470, 1-2471, 1-2472, 1-2473, 1-2474, 1-2475,1-2476, 1-2477, 1-2478, 1-2479, 1-2480, 1-2481, 1-2482, 1-2483, 1-2484,1-2485, 1-2486, 1-2487, 1-2488, 1-2489, 1-2490, 1-2491, 1-2492, 1-2493,1-2494, 1-2495, 1-2496, 1-2497, 1-2498, 1-2499, 1-2500, 1-2501, 1-2502,1-2503, 1-2504, 1-2505, 1-2506, 1-2507, 1-2508, 1-2509, 1-2510, 1-2511,1-2512, 1-2513, 1-2514, 1-2515, 1-2516, 1-2517, 1-2518, 1-2519, 1-2520,1-2521, 1-2522, 1-2523, 1-2524, 1-2525, 1-2526, 1-2527, 1-2528, 1-2529,1-2530, 1-2531, 1-2532, 1-2533, 1-2534, 1-2535, 1-2536, 1-2537, 1-2538,1-2539, 1-2540, 1-2541, 1-2542, 1-2543, 1-2544, 1-2545, 1-2546, 1-2547,1-2548, 1-2549, 1-2550, 1-2551, 1-2552, 1-2553, 1-2554, 1-2555, 1-2556,1-2557, 1-2558, 1-2559, 1-2560, 1-2561, 1-2562, 1-2563, 1-2564, 1-2565,1-2566, 1-2567, 1-2568, 1-2569, 1-2570, 1-2571, 1-2572, 1-2573, 1-2574,1-2575, 1-2576, 1-2577, 1-2578, 1-2657, 1-2665, 1-2667 and 1-2669.

The following compounds are even more preferred, that is Compounds No.:

1-46, 1-47, 1-48, 1-49, 1-50, 1-51, 1-52, 1-53, 1-54, 1-55, 1-56, 1-57,1-58, 1-59, 1-60, 1-61, 1-62, 1-63, 1-64, 1-65, 1-66, 1-67, 1-68, 1-69,1-70, 1-71, 1-271, 1-272, 1-273, 1-274, 1-275, 1-276, 1-277, 1-278,1-279, 1-280, 1-281, 1-282, 1-283, 1-284, 1-285, 1-286, 1-457, 1-458,1-459, 1-460, 1-461, 1-462, 1-463, 1-464, 1-465, 1-466, 1-467, 1-468,1-469, 1-470, 1-471, 1-472, 1-473, 1-474, 1-475, 1-476, 1-477, 1-478,1-479, 1-480, 1-481, 1-482, 1-483, 1-484, 1-485, 1-486, 1-487, 1-488,1-489, 1-490, 1-491, 1-492, 1-493, 1-494, 1-495, 1-496, 1-497, 1-498,1-499, 1-500, 1-501, 1-502, 1-503, 1-504, 1-505, 1-506, 1-507, 1-508,1-509, 1-510, 1-511, 1-512, 1-513, 1-514, 1-515, 1-516, 1-517, 1-518,1-519, 1-520, 1-521, 1-522, 1-523, 1-524, 1-525, 1-526, 1-527, 1-528,1-529, 1-530, 1-531, 1-532, 1-533, 1-534, 1-535, 1-536, 1-537, 1-538,1-539, 1-733, 1-734, 1-735, 1-736, 1-737, 1-738, 1-739, 1-740, 1-741,1-742, 1-743, 1-744, 1-745, 1-746, 1-747, 1-748, 1-749, 1-750, 1-815,1-820, 1-861, 1-1134, 1-1135, 1-1136, 1-1137, 1-1138, 1-1139, 1-1140,1-1141, 1-1142, 1-1143, 1-1144, 1-1145, 1-1146, 1-1147, 1-1148, 1-1224,1-1258, 1-1259, 1-1260, 1-1261, 1-1262, 1-1263, 1-1264, 1-1265, 1-1266,1-1267, 1-1268, 1-1269, 1-1270, 1-1271, 1-1272, 1-1273, 1-1274, 1-1275,1-1276, 1-1277, 1-1278, 1-1279, 1-1280, 1-1963, 1-1993, 1-2470, 1-2520,1-2566, 1-2567, 1-2568, 1-2569, 1-2570, 1-2571, 1-1272, 1-2573, 1-2574,1-2575, 1-2576, 1-2577, 1-2578, 1-2657, 1-2665, 1-2667 and 1-2669.

The following compounds are further preferred, that is Compounds No.:1-46, 1-47, 1-48, 1-49, 1-50, 1-71, 1-271, 1-496, 1-539, 1-733, 1-739,1-740, 1-741, 1-742, 1-815, 1-820, 1-861, 1-1135, 1-1145, 1-1224,1-1258, 1-1260, 1-1275, 1-1276, 1-1280, 1-1963, 1-1993, 1-2470, 1-2520,1-2567, 1-2665, 1-2667 and 1-2669.

The following compounds are particularly preferred, that is CompoundsNo.: 1-49, 1-271, 1-496, 1-539, 1-733, 1-738, 1-739, 1-740, 1-741,1-742, 1-820, 1-861, 1-1135, 1-1224, 1-1258, 1-1260, 1-1275, 1-1963,1-2470, 1-2520, 1-2567, 1-2657, 1-2665, 1-2667, and 1-2669.

The most preferred compounds are

N-[5-(1,2-Dithiolan-3-yl)pentanoyl]methanesulfonamide (Compound No.1-496);

Methyl 3-[4-(1,2-dithiolan-3-yl)butyl]ureidoacetate (Compounds No.1-739);

2(S)-{3-[4-[1,2-Dithiolan-3-yl)butyl]ureido}propionic acid (Compound No.1-740);

Methyl 2(S)-{3-[4-(1,2-dithiolan-3-yl)butyl[ureido}propionate (CompoundNo. 1-742);

Ethyl 3-[4-(1,2-dithiolan-3-yl)butyl]-1- methylureidoacetate (CompoundNo. 1-820 ethyl ester); and

N-[5-(1,2-Dithiolan-3-yl)pentyl]methanesulfonamide (Compound No.1-2470);

and pharmaceutically acceptable salts thereof.

The compounds of the present invention may be prepared by a variety ofmethods well known for the preparation of compounds of this generaltype. For example, they may be prepared by the following Methods A to G.

Method A

In this Method, a compound of formula (II) is reacted with a compound offormula (III), to give a compound of formula (Ia), which is a compoundof formula (I) in which the meanings of A and B are somewhat restricted.##STR8## In the above formulae: R¹, k, m and n are as defined above;

A¹ represents any of the groups defined above for A, other than thegroups of formula --CO--O--and --N(R²)O--[wherein R² is as definedabove];

B¹ represents a group of formula --N(R⁵)--or --N(R⁵)N(R⁶)--[wherein R⁵and R⁶ are as defined above]; and

Y represents a group to be eliminated.

There is no particular restriction on the group to be eliminated,provided that it can be eliminated as a nucleophilic residue, andexamples of such groups are well known to thos skilled in the art.Specific examples of such groups include:

halogen atoms, such as the chlorine, bromine and iodine atoms

trihalomethyl groups, such as the trichloromethyl group;

lower alkanesulfonyloxy groups, such as the methanesulfonyloxy andethanesulfonyloxy groups;

lower haloalkanesulfonyloxy groups, such as thetrifluoromethanesulfonyloxy and pentafluoroethanesulfonyloxy groups; and

arylsulfonyloxy groups, such as the benzenesulfonyloxy,p-toluenesulfonyloxy and p-nitrobenzenesulfonyloxy groups.

Of these, a halogen atom or an alkanesulfonyl group is preferred.

Step A1

In this Step, a dithiolan derivative of formula (Ia) is prepared byreacting a compound of formula (II) with a compound of formula (III) ina solvent in the presence of a base.

The reaction is normally and preferably effected in the presence of asolvent. There is no particular restriction on the nature of the solventto be employed, provided that it has no adverse effect on the reactionor on the reagents involved and that it can dissolve the reagents, atleast to some extent. Examples of suitable solvents include:

aromatic hydrocarbons, such as benzene, toluene and xylene; halogenatedhydrocarbons, such as methylene chloride, chloroform, carbontetrachloride, dichloroethane, chlorobenzene and dichlorobenzene;ethers, such as diethyl ether, diisopropyl ether, tetrahydrofuran,dioxane, dimethoxyethane and disthylene glycol dimethyl ether; ketones,such as acetone, methyl ethyl ketone, methyl isobutyl ketone, isophoroneand cyclohexanone; nitriles, such as acetonitrile, propionitrile andisobutyronitrile, amides, such a formamide, dimethylformamide,N,N-dimethylacetamide, N-methyl-2-pyrrolidone, N-methylpyrrolidinone andhexamethyl-phosphoric triamide; sulfoxides, such as dimethyl sulfoxide;and sulfones, such as sulfolane. Of these, we prefer the ketones, ethersand amides, more preferably acetone, tetrahydrofuran, dimethylformamideand N,N-dimethylacetamide.

There is likewise no particular restriction on the nature of the basesused, and any base commonly used in reactions of this type may equallybe used here. Examples of such bases include: inorganic bases, such asalkali metal carbonates (for example sodium carbonate, potassiumcarbonate, lithium carbonate or cesium carbonate), alkali metalhydrogencarbonates (for example sodium hydrogencarbonate, potassiumhydrogencarbonate or lithium hydrogencarbonate), alkali matals hydrides(for example lithium hydride, sodium hydride or potassium hydride),alkali metal or alkaline earth metal hydroxides (for example sodiumhydroxide, potassium hydroxide, barium hydroxide or lithium hydroxide)and alkali metal fluorides (for example sodium fluoride or potassiumfluoride); and alkali metal alkoxides (for example sodium sodiumethoxide, potassium methoxide, potassium ethoxide, potassium t-butoxideor lithium methoxide. Of these, the alkali metal carbonates, alkalimetal hydrides and alkali metal alkoxides are preferred, and potassiumcarbonate, sodium, hydride and potassium t-butoxide are most preferred.

The reaction can take place over a wide range of temperatures, and theprecise reaction temperature is not critical to the invention. Thepreferred reaction temperature will depend upon such factors as thenature of the solvent, and the starting material or reagent used.However, in general, we find it convenient to carry out the reaction ata temperature of from -20° C. to 100° C., more preferably from 0° C. to50° C. The time required for the reaction may also vary widely,depending on many factors, notably the reaction temperature and thenature of the reagents and solvent employed. However, provided that thereaction is effected under the preferred conditions outlined above, aperiod of from 10 minutes to 24 hours, more preferably from 30 minutesto 12 hours, will usually suffice.

Method B

This demonstrates the preparation of a compound of formula (Ib), that isa compound of formula (I) in which A represents an oxygen atom, or agroup of formula --N(R²)CO--, --N(R²)SO₂ --, --ON(R²)CO--, --ON(R²)SO₂--, --N(R²)N(R³)CO--, --(R²)N(R³)SO₂ --, --N(R²)CON(R³)N(R⁴)CO--,--N(R²)CON(R³)CO-- or --N(R²)CON(R³)SO₂ --[wherein R², R³ and R⁴ are asdefined above]. ##STR9##

In the above formulae:

B, R¹, Y, k, m and n are as defined above; and

A² represents an oxygen atom, or a group of formula --N(R²)CO--,--N(R²)SO₂ --, --ON(R²)CO--, --ON(R²)SO₂ --, --N(R²)N(R³)CO--,--(R²)N(R³)SO₂ --, --N(R²)CON(R³)N(R⁴)CO--, --N(R²)CON(R³)CO-- or--N(R²)CON(R³)SO₂ --[wherein R², R³ and R⁴ are as defined above].

Step B1

In this Step, a dithiolan derivative of formula (Ib) is prepared byreacting a compound of formula (IV) with a compound of formula (V) in asolvent in the presence of a base. The reaction is essentially the sameas that described above in Step A1, and may be carried out using thesame solvents, bases and reaction conditions.

Method C

This demonstrates the preparation of a compound of formula (Ic), that isa compound of formula (I) in which A represents a group of formula--N(R²)CO--, --N(R²)SO₂ --, --CON(R²)N(R³)CO--, --CON(R²)CO--,--CON(R²)SO₂ --, --O--CO--, --ON(R²)CO--, --ON(R²)SO₂ --,--O--CON(R²)N(R³)CO--, --O--CON(R²)CO--, --O--CON(R²)SO₂ --,--CO--CON(R²)N(R³)CO--, --CO--CON(R²)CO--, --CO--CON(R²)SO₂ --,--N(R²)CO--CO--, --N(R²)N(R³)CO--, --N(R²)N(R³)SO₂ --,--N(R²)CON(R³)N(R⁴)CO--, --N(R²)CON(R³)CO-- or --N(R²)CON(R³)SO₂--[wherein R², R³ and R⁴ are as defined above], and

B represents a single bond. ##STR10##

In the above formulae:

R¹, k, m and n are as defined above,

D¹ represents an oxygen atom, or a group of formula --N(R²)--,--CON(R²)--, --ON(R²)--, --O--CON(R²)--, --N(R²)N(R³)-- or--N(R²)CON(R³)--[wherein R² and R³ are as defined above],

E¹ represents a carbonyl group, a sulfonyl group or a group of formula--COCO--, and

Y' represents a group to be eliminated, as in the definition of Y;however, the imidazolyl group, or an active ester residue, includingacyloxy groups, such as the acetoxy group, or alkoxyacyloxy groups, suchas the methoxyacetoxy group, are preferred.

Step C1

In this Step, a dithiolan derivative of formula (Ic) is prepared byacylating or sulfonylating a compound of formula (VI) with a compound offormula (VII) in a solvent in the presence of a base.

The reaction is normally and preferably effected in the presence of asolvent. There is no particular restriction on the nature of the solventto be employed, provided that it has no adverse effect on the reactionor on the reagents involved and that it can dissolve the reagents, atleast to some extent. Examples of suitable solvents include: aromatichydrocarbons, such as benzene, toluene and xylene; halogenatedhydrocarbons, such as methylene chloride, chloroform, carbontetrachloride, dichloroethane, chlorobenzene and dichlorobenzene;ethers, such as diethyl ether, diisopropyl ether, tetrahydrofuran,dioxane, dimethoxyethane and diethylene glycol dimethyl ether; ketones,such as acetone, methyl ethyl ketone, methyl isobutyl ketone, isophoroneand cyclohexanone; nitriles, such as acetonitrile, propionitrile andisobutyronitrile; and amides, such as formamide, dimethylformamide,N,N-dimethylacetamide, N-methyl-2-pyrrolidone, N-methylpyrrolidinone andhexamethylphosphoric triamide. Of these, the aromatic hydrocarbons,halogentated hydrocarbons, ethers and amides are preferred, andhalogenated hydrocarbons, ethers and amides are more preferred.

There is likewise no particular restriction on the nature of the basesused, and any base commonly used in reactions of this type may equallybe used here. Examples of such based include: organic bases, such asN-methylmorpholine, triethylamine, tripropylamine, tributylamine,diisopropylethylamine, N-methyldicyclohexylamine, N-methylpiperidine,pyridine, 4-pyrrolidinopyridine, picoline,4-(N,N-dimethylamino)pyridine, pyridine,2,6-di(t-butyl)-4-methylpyridine, quinoline, N,N-dimethylaniline,N,N-diethylaniline, 1,5-diazabicyclo[4.3.0]non-5-ene (DBN),1,4-diazabicyclo[2.2.2]octane (DABCO) and1,8-diazabicyclo[5.4.0]undec-7-ene (DBU), of these, triethylamine anddiisopropylethylamine are preferred.

The reaction can take place over a wide range of temperatures, and theprecise reaction temperature is not critical to the invention. Thepreferred reaction temperature will depend upon such factors as thenature of the solvent, and the starting material or reagent used.However, in general, we fine it convenient to carry out the reaction ata temperature of from -20° C. to 100° C., more preferably from 0° C. to80° C. The time required for the reaction may also vary widely,depending on many factors, notably the reaction temperature and thenature of the reagents and solvent employed. However, provided that thereaction is effected under the preferred conditions outlined above, aperiod of from 5 minutes to 2 days, more preferably from 20 minutes to 1day, will usually suffice.

As an alternative, where the compound of formula (VI) is reacted with acompound of formula (VII) in which E¹ represents a carbonyl group, thereaction may also be accomplished using a compound of formula HOOC--R¹(wherein R¹ is as defined above) by reacting the compound of formula(VI) with the compound of formula (VII) using a condensing agent in asolvent in the presence or absence of a base.

There is no particular restriction on the nature of the condensingagents used, and any condensing agent commonly used in reactions of thistype may equally be used here. Examples of such condensing agentsinclude:

(1) a combination of a phosphoric acid ester, such as diethylcyanophosphate or diphenylphosphoryl azide, and the base describedbelow;

(2) a carbodiimide, such as 1,3-dicyclohexylcarbodiimide,1,3-diisopropylcarbodiimide or1-ethyl-3-(3-dimethylaminopropyl)carbodiimide; a combination of one ormore of the above carbodiimides and the base described below; acombination of one or more of the above carbodiimides and an N-hydroxycompound, such as N-hydroxysuccinimide, 1-hydroxybenzotriazole orN-hydroxy-5-norbornene-2,3-dicarboxyimide;

(3) a combination of a disulfide, such as 2,2'-dipyridyl disulfide or2,2'-dibenzothiazolyl disulfide, and a phosphine, such astriphenylphosphine or tributylphosphine;

(4) a carbonate, such as N,N'-disuccinimidyl carbonate, di-2-pyridylcarbonate or S,S'-bis(1-phenyl-1H-tetrozol-5-yl)dithiocarbonate;

(5) a phosphinic chloride, such asN,N'-bis(2-oxo-3-oxazolidinyl)phosphinic chloride;

(6) an oxalate, such as N,N'-disuccinimidyl oxalate, N,N'-diphthalimideoxalate, N,N'-bis(5-norbornene-2,3-dicarboxyimidyl)oxalate,1,1'-bis(benzotrialzolyl) oxalate, 1,1'-bis(6-chlorobenzotriazolyl)oxalate or 1,1'-bis(6-trifluoromethylbenzotriazolyl) oxalate;

(7) a combination of one or more of the above phosphines and anazodicarboxylic acid ester, such as diethyl azodicarboxylate, or anazodicarboxylic amide, such as 1,1'-(azodicarbonyl)dipiperidine; acombination of one or more of the above phosphines and the basedescribed below;

(8) an N-lower alkyl-5-arylisoxazolium-3'-sulfonate, such asN-ethyl-5-phenylisoxazolium-3'-sulfonate;

(9) a diheteroaryldiselenide, such as di-2-pyridyl diselenide;

(10) an arylsulfonyltriazolide, such asp-nitrobenzenesulfonyltriazolide;

(11) a 2-halo-1-lower alkylpyridinium halide, such as2-chloro-1-methylpyridinium iodide;

(12) an imidazole, such as 1,1'-oxalydiimidazole orN,N'-carbonyldiimidazole;

(13) a 3-lower alkyl-2-halobenzothiazolium fluoroborate such as3-ethyl-2-chloro-benzothiazolium fluoroborate;

(14) a 3-lower alkyl-benzothiazole-2-serone, such as3-methyl-benzothiazole-2-serone;

(15) a phosphate, such as phenyldichlorophosphate or polyphosphateester;

(16) a halosulfonyl isocyanate, such as chlorosulfonyl isocyanate;

(17) a halosilane, such as trimethylsilyl chloride or triethylsilylchloride;

(18) a combination of a lower alkanesulfonyl halide, such asmethanesulfonyl chloride and the base described below;

(19) an N,N,N',N'-tetra lower alkylhaloformamidium chloride, such asN,N',N'-tetramethylchloroformamidium chloride; and

(20) a combination of a lower alkyloxycarbonyl halide, such as ethylchlorocarbonate and the base described below;

preferably the above (1), (2), (7), (12) and (20).

The reaction is normally and preferably effected in the presence of asolvent. There is no particular restriction on the nature of the solventto be employed, provided that it has no adverse effect on the reactionor on the reagents involved and that it can dissolve the reagents, atleast to some extent. Examples of suitable solvents include: aliphatichydrocarbons, such as hexane and heptane; aromatic hydrocarbons, such asbenzene, toluene and xylene; halogenated hydrocarbons, such as methylenechloride, chloroform, carbon tetrachloride, dichloroethane,chlorobenzene and dichlorobenzene; esters, such as ethyl formate, ethylacetate, propyl acetate, butyl acetate and diethyl carbonate; ethers,such as diethyl ether, diisopropyl ether, tetrahydrofuran, dioxane,dimethoxyethane and diethylene glycol dimethyl ether; nitriles, such asacetonitrile and isobutyrontrile; and amides, such as formamide,dimethylformamide, N,N-dimethylacetamide, N-methyl-2-pyrrolidone,N-methylpyrrolidinone and hexamethylphosphoric triamide.

There is likewise no particular restriction on the nature of the basesused, and any base commonly used in reactions of this type may equallybe used here. Examples of such bases include: organic bases, such asN-methylmorpholine, triethylamine, tributylamine, diisopropylethylamine,dicyclohexylamine, N-methylpiperidine, pyridine, 4-pyrrolidinopyridine,picoline, 4-(N,N-dimethylamino)pyridine,2,6-di(t-butyl)-4-methylpyridine, quinoline, N,N-dimethylaniline andN,N-diethylaniline.

If desired, 4-(N,N-dimethylamino)pyridine and 4-pyrrolidinopyridine canbe combined with other bases and used in a catalytic amount. Also, inorder to carry out the reaction more effectively, a dehydrating agentsuch as a molecular sieve, a quaternary ammonium salt (for examplebenzyltriethylammonium chloride or tetrabutylammonium chloride), a crownether, such as dibenzo-18-crown-6, or an acid trapping agent, such as3,4-dihydro-2H-pyrido[1,2-1]pyrimidin-2-one, can be added to thereaction mixture.

The reaction can take place over a wide range of temperatures, and theprecise reaction temperature is not critical to the invention. Thepreferred reaction temperature will depend upon such factors as thenature of the solvent, and the starting material or reagent used.However, in general, we find it convenient to carry out the reaction ata temperature of from -20° C. to 80° C., more preferably from 0° C. toroom temperature. The time required for the reaction may also varywidely, depending on many factors, notably the reaction temperature andthe nature of the reagents and solvent employed. However, provided thatthe reaction is effected under the preferred conditions outlined above,a period of from 10 minutes to 3 days, more preferably from 30 minutesto 1 day, will usually suffice.

Method D

This demonstrates the preparation of a compound of formula (Id), that isa compound of formula (I) in which A represents a carbonyl group, or agroup of formula --CON(R²)N(R³)CO--, --CON(R²)CO--, --CON(R²)SO₂ --,--CO--O--, --CO--CON(R²)N(R³)CO--, --CO--CON(R²)CO-- or --CO--CON(R²)SO₂--[wherein R² and R³ are as defined above]. ##STR11##

In the above formulae:

B, R¹, Y', k, m and n are as defined above,

D² represents a carbonyl group or a group of formula --CO--CO--, and

E² represents an oxygen atom, or a group of formula --N(R²)N(R³)CO--,--N(R²)CO-- or --N(R²)SO₂ --[wherein R² and R³ are as defined above].

Step D1

In this Step, a dithiolan derivative of formula (Id) is prepared byacylating a compound of formula (IX) with a compound of formula (VIII)in a solvent in the presence of a base. The reaction is essentially thesame as that described above in Step C1, and may be carried out usingthe same solvents, bases and reaction conditions.

Alternatively, the dithiolan derivative of formula (Id) can be preparedby reacting a compound of formula (VIII') with the compound of formula(IX) using a condensing agent in a solvent in the presence or absence ofa base. ##STR12## (wherein D², k, m and n are as defined above.)

The reaction is normally and preferably effected in the presence of asolvent. There is no particular restriction on the nature of the solventto be employed, provided that it has no adverse effect on the reactionor on the reagents involved and that it can dissolve the reagents, atleast to some extent. Examples of suitable solvents include: aliphatichydrocarbons, such as hexane and heptane; aromatic hydrocarbons, such asbenzene, toluene and xylene; halogenated hydrocarbons, such as methylenechloride, chloroform, carbon tetrachloride, dichloroethane,chlorobenzene and dichlorobenzene; esters, such as ethyl formate, ethylacetate, propyl acetate, butyl acetate and diethyl carbonate; ethers,such as diethyl ether, diisopropyl ether, tetrahydrofuran, dioxane,dimethoxyethane and diethylene glycol dimethyl ether; nitriles, such asacetonitrile and isobutyrontrile; and amides, such as formamide,dimethylformamide, N,N-dimethylacetamide, N-methyl-2-pyrrolidone,N-methylpyrrolidinone and hexamethylphosphoric triamide.

There is likewise no particular restriction on the nature of the basesused, and any base commonly used in reactions of this type may equallybe used here. Examples of such bases include: organic bases, such asN-methylmorpholine, triethylamine, tributylamine, diisopropylethylamine,dicyclohexylamine, N-methylpiperidine, pyridine, 4-pyrrolidinopyridine,picoline, 4-(N,N-dimethylamino)pyridine,2,6-di(t-butyl)-4-methylpyridine, quinoline, N,N-dimethylaniline andN,N-diethylaniline.

If desired, 4-(N,N-dimethylamino)pyridine and 4-pyrrolidinopyridine canbe combined with other bases and used in a catalytic amount. Also, inorder to carry out the reaction more effectively, a dehydrating agentsuch as a molecular sieve, a quaternary ammonium salt (for examplebenzyltriethylammonium chloride or tetrabtylammonium chloride), a crownether, such as dibenzo-18-crown-6, or an acid trapping agent, such as3,4-dihydro-2H-pyrido[1,2-1]pyrimidin-2-one, can be added to thereaction mixture.

The reaction can take place over a wide range of temperatures, and theprecise reaction temperature is not critical to the invention. Thepreferred reaction temperature will depend upon such factors as thenature of the solvent, and the starting material or reagent used.However, in general, we find it convenient to carry out the reaction ata temperature of from -20° C. to 80° C., more preferably from 0° C. toroom temperature. The time required for the reaction may also varywidely, depending on many factors, notably the reaction temperature andthe nature of the reagents and solvent employed. However, provided thatthe reaction is effected under the preferred conditions outlined above,a period of from 10 minutes to 3 days, more preferably from 30 minutesto 1 day, will usually suffice.

Method E

This demonstrates the preparation of a compound of formula (Ie), that isa compound of formula (I) in which:

A represents a group of formula --N(R²)CO--[wherein R² represents ahydrogen atom], and

B represents a group of formula --N(R⁵)-- or --N(R⁵)N(R⁶)--[wherein R⁵and R⁶ are as defined above]. ##STR13##

In the above formulae: B¹, R¹, k, m and n are as defined above.

Step E1

In this Step, an isocyanic acid ester of formula (XI) is prepared byazidating the carboxy group of a compound of formula (X) in a solvent inthe presence or absence of a catalyst to obtain an acid azide compoundand then heating it.

The azidation reaction is normally and preferably effected in thepresence of a solvent. There is no particular restriction on the natureof the solvent to be employed, provided that it has no adverse effect onthe reaction or on the reagents involved and that it can dissolve thereagents, at least to some extent. Examples of suitable solventsinclude: aromatic hydrocarbons, such as benzene, toluene and xylene;halogenated hydrocarbons, such as methylene chloride and chloroform;ethers, such as diethyl ether, tetrahydrofuran, dioxane anddimethoxyethane; nitriles, such as acetonitrile; and amides, such asformamide, dimethylformamide, N,N-dimethylacetamide,N-methyl-2-pyrrolidone, N-methylpyrrolidinone and hexamethylphosphorictriamide. Of these, we prefer the aromatic hydrocarbons, the halogenatedhydrocarbons and the ethers.

There is likewise no particular restriction on the nature of theazidation agents used, an any azidation agent commonly used in reactionsof this type may equally be used here. Examples of such azidation agentsinclude: diarylphosphoryl azide derivatives, such as diphenylphosphorylazide; trialkylsilyl azides, such as trimethylsilyl azide ortriethylsilyl azide; and alkali metal salt azides, such as sodium azide,potassium azide or lithium azide. Of these, we prefer thediarylphosphoryl azide derivatives.

There is likewise no particular restriction on the nature of thecatalysts used, and any catalyst commonly used in reactions of this typemay equally be used here. Examples of such catalysts include: Lewisacids, such as trialkylsilyl triflates (e.g. trimethylsilyl triflate andtriethysilyl triflate), trifluoroborane etherate, aluminum chloride andzinc chloride; and organic bases, such as N-methylmorpholine,triethylamine, tributylamine, diisopropylethylamine, dicyclohexylamine,N-methylpiperidine, pyridine, 4-pyrrolidinopyridine, picoline,4-(N,N-dimethylamino)pyridine, 2,6-di-t-butyl-4-methylpyridine,quinoline, N,N-dimethylaniline and N,N-diethylaniline.

The reaction can take place over a wide range of temperatures, and theprecise reaction temperature is not critical to the invention. Thepreferred reaction temperature will depend upon such factors as thenature of the solvent, and the starting material or reagent used.However, in general, we find it convenient to carry out the reaction ata temperature of from 20° C. to 180° C., more preferably from 50° C. to150° C. The time required for the reaction may also vary widely,depending on many factors, notably the reaction temperature and thenature of the reagents and solvent employed. However, provided that thereaction is effected under the preferred conditions outlined above, aperiod of from 10 minutes to 24 hours, more preferably from 30 minutesto 8 hours, will usually suffice.

Step E2

In this Step, a dithiolan derivative of formula (Ie) is prepared byreacting an isocyanic acid ester (XI) with a compound of formula (XII)in a solvent.

The reaction is normally and preferably effected in the presence of asolvent. There is no particular restriction on the nature of the solventto be employed, provided that it has no adverse effect on the reactionor on the reagents involved and that it can dissolve the reagents, atleast to some extent. Examples of suitable solvents include: aromatichydrocarbons, such as benzene, toluene and xylene; halogenatedhydrocarbons, such as methylene chloride, chloroform, carbontetrachloride, dichloroethane, chlorobenzene and dichlorobenzene;ethers, such as diethyl ether, diisopropyl ether, tetrahydrofuran,dioxane, dimethoxyethane and diethylene glycol dimethyl ether; ketones,such as acetone, methyl ethyl ketone, methyl isobutyl ketone, isophoroneand cyclohexanone; nitriles, such as acetonitrile, propionitrile andisobutyronitrile; and amides, such as formamide, dimethylformamide,N,N-dimethylacetamide, N-methyl-2-pyrrolidone, N-methylpyrrolidinone andhexamethylphosphoric triamide; sulfoxides, such as dimethyl sulfoxide;and sulfones, such as sulfolane. Of these, we prefer the aromatichydrocarbons, halogenated hydrocarbons, ethers, nitriles and amides,more preferably the aromatic hydrocarbons, halogentated hydrocarbons,ethers, nitriles and amides.

The reaction can take place over a wide range of temperatures, and theprecise reaction temperature is not critical to the invention. Thepreferred reaction temperature will depend upon such factors as thenature of the solvent, and the starting material or reagent used.However, in general, we fine it convenient to carry out the reaction ata temperature of from -20° C. to 100° C., more preferably from 0° C. to80° C. The time required for the reaction may also vary widely,depending on many factors, notably the reaction temperature and thenature of the reagents and solvent employed. However, provided that thereaction is effected under the preferred conditions outlined above, aperiod of from 5 minutes to 2 days, more preferably from 20 minutes to 1day, will usually suffice.

Alternatively, the compound of formula (I) in which A represents a groupof formula --N(R²)CON(R³)N(R⁴)CO--, --N(R²)CON(R³)CO-- or--N(R²)CON(R³)SO₂ --[wherein R² represents a hydrogen atom, and R³ andR⁴ are as defined above]can be prepared by reacting the above isocyanicacid ester of formula (XI) with a compound of formula: H--D³ --B--R¹{wherein B and R¹ are as defined above, and D³ represents a group offormula --N(R³)N(R⁴)CO--, --N(R³)CO-- or --N(R³)SO₂ --[wherein R³ and R⁴are as defined above]}, following the same procedure as described above.

A compound of formula (I) in which A represents a group of formula--N(R²)CO-- (wherein R² represents a hydrogen atom), B represents asingle bond, and R¹ represents a group OR⁷ (wherein R⁷ is as definedabove) can be prepared by reacting the above isocyanic acid ester offormula (XI) with a compound of formula: HOR⁷ (wherein R⁷ is as definedabove), following the same procedure as described above.

A hydrogen atom of an amino, amide or imide group can be replaced byanother group by reacting a compound of formula (I) in which R², R³, R⁴,R⁵ and/or R⁶ represent a hydrogen atom with a compound of formula: Y--R⁸(in which Y is as defined above and R⁸ represents a group other than ahydrogen atom in the definition of R², R³, R⁴ and R⁶) according to theabove Method A, or by alkylation using a combination of an alcohol and acarbodiimide, such as dicyclohexylcarbodiimide. For example, after thedithiolan derivative of the present invention is synthesized accordingto the above Method E, a hydrogen atom of an amide group in the compoundcan be replaced by another group by these processes.

Method F

This demonstrates the preparation of a compound of formula (If), that isa compound of formula (I) in which:

A represents a group of formula --O--CO--, --N(R²)CO--, --N(R²)CS--,--CON(R²)CO--, --CON(R²)CS--, --ON(R²)CO--, --O--CON(R²)CO--,--N(R²)N(R³)CO-- or --N(R²)CON(R³)CO--[wherein R² and R³ are as definedabove],

B represents a single bond or a group of formula --N(R^(5'))--[whereinR^(5') represents the groups other than hydrogen in the definition ofR⁵⁻ ], and

R¹ represents a group as defined above other than hydrogen. ##STR14##

In the above formulae:

D¹, k, m and n are as defined above,

E³ represents a single bond or a group of formula --N(R^(5'))--[whereinR^(5') is as defined above],

G represents an oxygen atom or a sulfur atom, and

R^(1') represents a group as defined above for R¹ other than hydrogen.

Step F1

In this Step, a dithiolan derivative of formula (If) is prepared byreacting an isocyanic acid ester or an isothiocyanic acid ester offormula (XIII) with a compound of formula (VI). The reaction isessentially the same as that described above in Step E2, and may becarried out using the same solvents, bases and reaction conditions.

The compound of formula (If) wherein E³ represents a single bond andR^(1') represents a hydrogen atom can also be prepared by carrying outthe reaction using a compound of formula G═CN--R⁹ [wherein G is asdefined above and R⁹ represents a silyl group, such as a tri-loweralkylsilyl group, e.g. trimenthylsilyl, triethylsilyl,isopropyldimethylsilyl, t-butyldimenthylsilyl, methyldiisopropylsilyl,methyldi-t-butylsilyl or triisopropylsilyl, or a tri-lower alkylsilylgroup substituted with 1 or 2 aryl groups, such as adiphenylmethylsilyl, diphenylbutylsilyl, diphenylisopropylsilyl orphenyldiisopropylsilyl group]instead of the isocyanic acid ester or theisothiocyanic acid ester of formula (XIII).

Where the dithiolan ring is subjected to ring-opening in the course ofcarrying out the reactions described in Methods A to F to produce adithiol compound, a dithiolan derivative can be obtained by oxidizingthe ring-opening compound to form a disulfide bond. The oxidationreaction is usually carried out using an oxidizing agent in the presenceof a solvent.

The reaction is normally and preferably effected in the presence of asolvent. There is no particular restriction on the nature of the solventto be employed, provided that it has no adverse effect on the reactionor on the reagents involved and that it can dissolve the reagents, atleast to some extent. Preferred solvents include water-containingorganic solvents. Such organic solvent include: ketones, such asacetone; halogenated hydrocarbons, such as methylene chloride,chloroform or carbon tetrachloride; nitriles, such as acetonitrile;ethers, such as diethyl ether, tetrahydrofuran and dioxane; amides, suchas dimethylformamide, dimethylacetamide or hexamethylphosphorictriamide; sulfoxides, such as dimethyl sulfoxide; and alcohols, such asmethanol or ethanol.

There is likewise no particular restriction on the nature of theoxidizing agents used, and any oxidizing agent commonly used inreactions of this type may equally be used here provided it can form adisulfide bond. Examples of such oxidizing agents include ferricchloride.

The reaction can take place over a wide range of temperatures, and theprecise reaction temperature is not critical to the invention. Thepreferred reaction temperature will depend upon such factors as thenature of the solvent, and the starting material or reagent used.However, in general, we find it convenient to carry out the reaction ata temperature of from 0 to 150° C. The time required for the reactionmay also vary widely, depending on many factors, notably the reactiontemperature and the nature of the reagents and solvent employed.However, provided that the reaction is effected under the preferredconditions outlined above, a period of from 10 minutes to 24 hours willusually suffice.

Method G

This illustrates the preparation of a compound of formula (I) in whichat least one of m and n is 1 or 2, that is a compound of formula (Ig)from a compound of formula in which m and n are both zero, that is acompound of formula (Ig'). ##STR15##

In the above formulae:

A, B, R¹ and k are as defined above; and

m' and n' are as defined above for m and n provided that at least one isnot 0.

Step G1

In this Step, a dithiolan derivative of formula (Ig) is prepared byoxidizing a compound of formula (Ig') [a compound of formula (I) whereinn and m are 0].

There is no particular restriction on the nature of the oxidizing agentsused, and any oxidizing agent commonly used in reactions of this typemay equally be used here, provided that it is capable of oxidising asulfide to a sulfoxide or a sulfone. Examples of such oxidizing agentsinclude: hydroperoxides, such as hydrogen peroxide, t-butylhydroperoxide or pentyl hydroperoxide; dialkyl peroxides, such asdi-t-butyl peroxide; peracids, such as perbenzoic acid,m-chloroperbenzoic acid or peracetic acid; peracid esters, such asmethyl perbenzoate; and diacyl peroxides, such as benzoyl peroxide. Ofthese, we particularly prefer hydrogen peroxide, m-chloroperbenzoic acidand t-butyl hydroperoxide.

The reaction is normally and preferably effected in the presence of asolvent. There is no particular restriction on the nature of the solventto be employed, provided that it has no adverse effect on the reactionor on the reagents involved and that it can dissolve the reagents, atleast to some extent. Examples of suitable solvents include: aromatichydrocarbons, such as benzene, toluene and xylene; halogenatedhydrocarbons, such as methylene chloride, chloroform, carbontetrachloride, dichloroethane, chlorobenzene and dichlorobenzene;ethers, such as diethyl ether, diisopropyl ether, tetrahydrofuran,dioxane, dimethoxyethane and diethylene glycol dimethyl ether; ketones,such as acetone, methyl ethyl ketone, methyl isobutyl ketone, isophoroneand cyclohexanone; nitriles, such as acetonitrile, propionitrile andisobutyronitrile; and amides, such as formamide, dimethylformamide,N,N-dimethylacetamide, N-methyl-2-pyrrolidone, N-methylpyrrolidinone andhexamethylphosphoric triamide; sulfoxides, such as dimethyl sulfoxide;sulfones, such as sulfolane; alcohols, such as methanol and ethanol;esters, such as ethyl formate, ethyl acetate, propyl acetate, butylacetate and diethyl carbonate; and water. Of these, we prefer thearomatic hydrocarbons, halogenated hydrocarbons, ketones, amides,alcohols and water, more preferably the halogenated hydrocarbons,ketones, amides, alcohols and water.

The reaction can take place over a wide range of temperatures and theprecise reaction temperature is not critical to the invention. Thepreferred reaction temperature will depend upon such factors as thenature of the solvent, and the starting material or reagent used.However, in general, we find it convenient to carry out the reaction ata temperature of from -50 to 100° C., more preferably from -20 to 50° C.The time required for the reaction may also vary widely, depending onmany factors, notably the reaction temperature and the nature of thereagents and solvent employed. However, provided that the reaction iseffected under the preferred conditions outlined above, a period of from10 minutes to 2 days, more preferably from 30 minutes to 12 hours, willusually suffice.

After completion of each of the above reactions, the desired compoundmay be recovered from the reaction mixture by conventional methods.

For example, the desired compound may be obtained by: suitablyneutralising the reaction mixture; removing insolubles by filtration ifinsolubles exist; adding a water-immiscible organic solvent, such asethyl acetate to the reaction mixture; washing with water or anothersuitable solvent; separating the organic layer containing the desiredcompound; drying it over a drying agent, such as anhydrous sodiumsulfate or anhydrous magnesium sulfate; and removing the solvent, e.g.by evaporation.

The compound thus obtained can be separated and purified, if necessary,by appropriately combining conventional methods, for example,recrystallization, reprecipitation or other methods commonly used in theseparation and purification of organic compounds, for example,adsorption column chromatography using a carrier such as silica gel,alumina or magnesium-silica gel type Florisil; a method using asynthesized adsorbent such as partition column chromatography using acarrier such as Sephadex LH-20 (™, manufactured by Pharmacia Co, Ltd.),Amberlite XAD-11 (™, manufactured by Rohm and Haas Co. Ltd.) and DiaionHP-20 (™, manufactured by Mitsubishi Kasei Corporation), a method usingan ion exchange chromatogram, or normal phase or reverse phase columnchromatography using silica gel or alkylated silica gel (preferably highperformance liquid chromatography), and eluting with a suitable eluent.

The starting materials in Methods A to G are known compounds or arecompounds synthesized from known compound by conventional methods. Forexample, the amino derivative of formula (Ih), which is a startingmaterial in Method A, Method C and Method F can be prepared by thefollowing Method H.

Method H ##STR16##

In the above formulae: k, m, and n are as defined above.

Step H1

In this Step, a phthalimide derivative of formula (XVI) is prepared bycarrying out a Mitsunobu reaction between a compound of formula (XIV)and phthalimide of formula (XV).

There is no particular restriction on the nature of the reagents used inthe Mitsunobu reaction, and any reagent commonly used in reactions ofthis type may equally be used here. Examples of such reagents include: acombination of an azo compound, such as a di-lower alkylazodicarboxylate (for example dimethyl azodicarboxylate, diethylazodicarboxylate or diisopropyl azodicarboxylate) or an azodicarboxamide[such as 1,1'-(axodicarbonyl)dipiperidine] and a phosphine, such as atriarylphosphine (for example triphenylphosphine) or a tri-lower alkylphosphine (for example tributylphosphine), more particularly acombination of a di-lower alkyl azodicarboxylate and a triarylphosphine,most preferably a combination of dimethyl azodicarboxylate andtriphenylphosphine.

The reaction is normally and preferably effected in the presence of asolvent. There is no particular restriction on the nature of the solventto be employed, provided that it has no adverse effect on the reactionor on the reagents involved and that it can dissolve the reagents, atleast to some extent. Examples of suitable solvents include: aromatichydrocarbons, such as benzene, toluene and xylene; halogenatedhydrocarbons, such as methylene chloride, chloroform, carbontetrachloride, dichloroethane, chlorobenzene and dichlorobenzene;esters, such as ethyl formate, ethyl acetate, propyl acetate, butylacetate and diethyl carbonate; ethers, such as diethyl ether,diisopropyl ether, tetrahydrofuran, dioxane, dimethoxyethane anddiethylene glycol dimethyl ether; nitriles, such as acetonitrile andisobutyronitrile; amides, such as formamide, dimethylformamide,N,N-dimethylacetamide, N-methyl-2-pyrrolidone, N-methylpyrrolidinone andhexamethylphosphoric triamide; and sulfoxides, such as dimethylsulfoxide and sulfolane. Of these, we prefer the aromatic hydrocarbonsand ethers.

The reaction can take place over a wide range of temperatures, and theprecise reaction temperature is not critical to the invention. Thepreferred reaction temperature will depend upon such factors as thenature of the solvent, and the starting material or reagent used.However, in general, we find it convenient to carry out the reaction ata temperature of from -20 to 100° C., more preferably from 0 to 50° C.The time required for the reaction may also vary widely, depending onmany factors, notably the reaction temperature and the nature of thereagents and solvent employed. However, provided that the reaction iseffected under the preferred conditions outlined above, a period of from10 minutes to 3 days, more preferably from 30 minutes to 12 hours, willusually suffice.

Step H2

In this Step, an amino derivative of formula (Ih) is prepared byreacting the phthalimide derivative of formula (XVI) with butylamine orhydrazine in a solvent. For example it may be accomplished by reactingthe phthalimide derivative of formula (XVI) with butylamine in methanolat room temperature for 6 hours.

Since the dithiolan derivatives have the effect of increasing theactivity of glutathione reductase, a composition which increases theactivity of glutathione reductase, containing those compounds orpharmaceutically acceptable salts thereof can be used for the preventionor treatment of diseases resulting from oxidative stress. Examples ofdiseases resulting from oxidative stress are disease or pathologicstates including damage caused by alcohol abuse, exposure to xenobioticagents or radiation; intracellular oxidative states caused by hepaticdiseases; intoxication from drugs and chemical agents (e.g. carcinostatsincluding platinum chelate, antibiotics, antiparasitics, paraquat,carbon tetrachloride and halothane); intoxication from heavy metals;disorders of the nervous system including brain and neurone degenerativedisorders (e.g. cerebral ischemia, cerebral ictus, hypoglycemia,epileptic attacks, amyotrophic lateral schlerosis, Alzheimer's disease,Parkinson's disease and Huntington's chorea); diseases related to analtered functionality of the immune system, in particular tumourimmunotherapy; infertility, in particular male infertility; coronaryheart disease, ophthalmologic disorders such as cataract, retinopathy ofprematurity and siderosis; pulmonary diseases such as idiopathicpulmonary fibrosis, adult respiratory distress syndrome, emphysema,asthma, bronchopulmonary dysplasia and interstitial pulmonary fibrosis;chronic renal failure; gastric ulcer; canceration and metastases ofcancer including colorectal cancer; diabetes; hepatocyte necrosis andapoptosis including ethanol-induced hepatopathy; viral diseasesincluding influenza, hepatitis B and HIV; abnormalities of blood orblood vessels such as Fanconi's anemia, septicemia, enhancedpermeability through blood vessels and leukocyte adherence; variousmalformations such as Down's syndrome, Duchenne muscular dystrophy,Becker dystrophy, Dubin-Johnson-Spring syndrome and favism; andinflammatory diseases such as nephritis, pancreatitis, dermatitis,fatigue and rheumatism. In particular, the dithiolan derivatives andpharmaceutically acceptable salts thereof of the present invention areuseful for the prevention or treatment of diseases or pathologic statessuch as damage caused by radiation, intracellular oxidative statescaused by hepatic diseases, intoxication (i.e. side effects) fromcarcinostats including platinum chelate, disorders of the nervoussystem, cataract, diabetes, hepatocyte necrosis and apoptosis, viraldiseases, and inflammatory diseases.

Among the above-described diseases resulting from oxidative stress,there are some diseases where the effects are irreversible, once theyhave occurred. A therapeutic agent for such a disease means a medicamentwhich prevents or delays the progress of the disease.

The dithiolan derivatives of formula (I) or pharmaceutically acceptablesalts thereof of the present invention can be used together with amedicament which is known as a preventive agent or therapeutic agent fora disease listed above as the diseases resulting from oxidative stressand may show a synergistic effect.

Cyanamide, disulfiram, adenine and cysteine are known as medicaments fortreating the damage caused by alcohol abuse, exposure to xenobioticagents or radiation; aminoethylsulfonic acid, protoporphyrin disodiumand diisopropylamine dichloroacetate are known as medicaments fortreating intracellular oxidative states caused by hepatic diseases;gluthathione, dimercaprol, and calcium disodium edetate are known asmedicaments for treating intoxication from drugs and chemical agents(e.g. carcinostats including platinum chelate, antibiotics,antiparasitics, paraquat, carbon tetrachloride and halothane) or fortreating intoxication from heavy metals; phenobarbital, phenytoin,bromocriptine mesylate, sulpiride, sodium valproate, haloperidol,levodopa-carbidopa, idebenone and aniracetam are known as medicamentsfor treating disorders of the nervous system including brain and neuronedegenerative disorders (e.g. cerebral ischemia, cerebral ictus,hypoglycemia, epileptic attacks, amyotrophic lateral sclerosis,Alzeimer's disease, Parkinson's disease and Huntington's chorea);cyclophosphamide, interferon-α and interferon-β are known as medicamentsfor treating diseases related to an altered functionality of the immunesystem, in particular tumour immunotherapy; sildenafil is known as amedicament for treating infertility, in particular male infertility;digitoxin and digoxin are known as medicaments for treating coronaryheart disease; pirenoxine is known as a medicament for treatingophtalmologic disorders such as cataract, retinopathy of prematurity andsiderosis; theophylline, ketotifen fumarate, epinastine hydrochloride,pranlukast and suplatast tosylate are known as medicaments for treatingpulmonary diseases such as idiopathic pulmonary fibrosis, adultrespiratory distress syndrome, emphysema, asthma, bronchopulmonarydysplasia and interstitial pulmonary fibrosis; furosemide, etacrynicacid and bumetanide are known as medicaments for treating chronic renalfailure; teprenone, rebamipide, ecabet sodium, plaunotol, famotidine,ranitidine hydrochloride and lansoprazole are known as medicaments fortreating gastric ulcer; BB-2516 and AG3340 are known to be usefulagainst canceration and metastases of cancer including colorectalcancer, epalrestat, voglibose, acarbose, insulin, glibenclamide andtroglitazone are known as medicaments for treating diabetes;aminoethylsulfonic acid, protoporphyrin disodium and diisopropylaminedichloroacetate are known as medicaments for treating hepatocytenecrosis and apoptosis including ethanol-induced hepatopathy; acyclovir,zidovudine, interferon-α, interferon-β and interferon-γ are known asmedicaments for treating viral diseases including influenza, hepatitis Band HIV; erythropoietin derivatives are known as medicaments fortreating abnormalities of the blood or blood vessels such as Fanconi'sanemia, septicemia, enhanced permeability through blood vessels andleukocyte adherence; fenipentol, camostat mesylate, indomethacin,loxoprofen sodium and diclofenac sodium are known as medicaments fortreating inflammatory diseases such as nephritis, pancreatitis,dermatitis, fatigue and rheumatism.

The compounds of the present invention can be administered in anyconventional pharmaceutical formulation, the nature of which will dependon the patient and the intended route of administration. For example fororal administration, suitable formulations include tablets, capsules,granules, powders or syrups. For parenteral administration suitableformulations include injections or suppositories. These formulations canbe prepared by well-known methods using additives such as excipients,lubricants, binders, disintegrating agents, stabilizers, corrigents anddiluents.

Examples of suitable excipients include organic excipients, for example:sugar derivatives such as lactose, sucrose, glucose, mannitol orsorbitol; starch derivatives such as corn starch, potato starch,α-starch, dextrin or carboxymethyl starch; cellulose derivatives such ascrystalline cellulose, low substituted hydroxypropylcellulose,hydroxypropylmethylcellulose, carboxymethylcellulose,carboxymethylcellulose calcium or internally bridgedcarboxymethylcellulose sodium; gum arabic; dextran; and Pullulan;inorganic excipients including silicate derivatives such as lightsilicic acid anhydride, synthetic aluminum silicate or magnesiummeta-silica acid aluminate; phosphates such as calcium phosphate;carbonates such as calcium carbonate; and sulfates such as calciumsulfate.

Examples of suitable lubricants include stearic acid, metal stearatessuch as calcium stearate or magnesium; talc; colloidal silica; waxessuch as beeswax or spermaceti; boric acid; adipic acid; sulfates such assodium sulfate; glycol; fumaric acid; sodium benzoate; DL-leucine;sodium salts of fatty acids; lauryl sulfates such as sodium laurylsulfate or magnesium lauryl sulfate; silicates such as silicic acidanhydride or silicic acid hydrate; and the foregoing starch derivatives.

Examples of suitable binders include polyvinylpyrrolidone, Macrogol, andsimilar compounds to the excipients described above.

Examples of suitable disintegrating agents include similar compounds tothe excipients described above; and chemically modified starches orcelluloses such as crosscarmelose sodium, sodium carboxymethylstarch orbridged polyvinylpyrrolidone.

Examples of suitable stabilisers include paraoxybenzoates such asmethylparaben or propylparaben; alcohols such as chlorobutanol, benzylalcohol or phenylethyl alcohol; benzalkonium chloride; phenols such asphenol or cresol; thimerosal; dehydroacetic acid; and sorbic acid.

Examples of suitable corrigents include sweeteners, vinegar or perfumessuch as those conventionally used.

Moreover, since the dithiolan derivative or the pharmaceuticallyacceptable salt thereof of the present invention is less stimulating forthe eyes, it can be topically administered to the eyes. Suitableformulations for the topical administration to the eyes includesolutions, suspensions, gels, ointments and solid inserting agents.

The formulation of these compositions for topical administration maycontain the dithiolan derivative or the pharmaceutically acceptable saltthereof at a level of from 0.001% (preferably 0.01%) as a lower limit to10% (preferably 5%) as an upper limit.

The pharmaceutical formulation containing an active compound can, ifdesired, be mixed with a non-toxic inorganic or organic carrier forpharmaceuticals.

Typical pharmaceutically acceptable carriers include water, a mixture ofwater and a water-miscible solvent such as a lower alkanol or aralkanol,a vegetable oil, polyalkylene glycol, a jelly using a petroleum as abase material, ethylcellulose, ethyl oleate, carboxymethylcellulose,polyvinylpyrrolidone, isopropyl myristate and other acceptable carrierswhich can be preferably used. The formulation may contain non-toxicauxiliary substances such as an emulsifier, a preservative, a wettingagent and an excipient, for example, polyethylene glycol 200, 300, 400and 600, carbowax 1000, 1500, 4000, 6000 and 10000, ρ-hydoxybenzoic acidesters such as methyl ρ-hydroxybenzoate or propyl ρ-hydroxybenzoate, aquaternary ammonium compound (for example, benzetonium chloride orbenzalkonium chloride) which are known as compounds having anti-fungalproperties at low temperatures and are non-toxic when used, ananti-fungal agent such as a phenyl mercury salt, a buffering componentsuch as thimerosal, methyl- and propylparaben, benzyl alcohol,phenylethanol, sodium chloride, sodium borate and sodium acetate, agluconic acid buffering agent and sorbitan monolaurate, triethanolamine,polyoxyethylenesorbitan monopalmitate, sodium dioctyl sulfosuccinate,monothioglycerol, thiosorbitol and ethylenediaminetetraacetic acid.

Ophthalmological excipients can be used as a desired support medium forthe compounds of the present invention and examples include the usualphosphoric acid buffering excipients (for example, a sodium phosphatebuffer or a potassium phosphate buffer), isotonic boric acid excipients,isotonic sodium chloride excipients and isotonic sodium borateexcipients.

As a further alternative, the pharmaceutical formulation may have theform of a solid insert which remains almost intact after the formulationhas been administered, or it may also be formulated as a disintegratinginsert which dissolves in the tear fluid or is disintegrated by othermethods.

The dose of the dithiolan derivative of formula (I) or thepharmaceutically acceptable salt thereof of the present invention willvary, depending upon the condition and age of the patient and the formand route of administration. However, for example, in the case of oraladministration, for an adult human patient, it is desirable toadminister from 0.1 mg (preferably 1 mg) as a lower limit to 10000 mg(preferably 5000 mg) as an upper limit per day. In the case ofintravenous administration, it is desirable to administer from 0.01 mg(preferably 0.1 mg) as a lower limit to 5000 mg (preferably 2000 mg) asan upper limit per day. In the case of topical administration to theeyes, it is desirable to administer from 0.001 mg (preferably 0.01 mg)as a lower limit to 500 mg (preferably 200 mg) as an upper limit perday. All of the above may be administered as a single dose or in divideddoses. The dose and dosage regime will depend on the condition of thepatient.

Pharmaceutical preparations of the present invention are illustrated bythe following non-limiting Formulation Examples.

FORMULATION EXAMPLE 1

Powder

5 g of N-[5-(1,2-dithiolan-3-yl)pentanoyl]methanesulfonamide (thecompound of Example 2 hereafter), 895 g of lactose and 100 g or cornstarch are mixed by means of a blender to obtain a powder.

FORMULATION EXAMPLE 2

Granules

5 g of N-[5-(1,2-dithiolan-3-yl)pentanoyl]sulfamide (the compound ofExample 7 hereafter), 865 g of lactose and 100 g of low substitutedhydroxypropylcellulose are mixed. 300 g of a 10% w/v aqueous solution ofhydoxypropyl cellulose are then added to the mixture, and then theresulting mixture is kneaded. The mixture is then granulated using anextruding granulator, after which it is dried to obtain a granuleformulation.

FORMULATION EXAMPLE 3

Capsules

5 g of N-[4-(1,2-dithiolan-3-yl)butyl-N'-methylurea (the compound ofExample 8 hereafter), 115 g of lactose, 58 g of corn starch and 2 g ofmagnesium stearate are mixed using a V-type mixer. 180 mg of the mixtureare then encapsulated in a No. 3 capsule to obtain a capsuleformulation.

FORMULATION EXAMPLE 4

Tablet

5 g of (R)-N-[5-(1,2-dithiolan-3-yl) pentanoyl]methanesulfonamide (thecompound of Example 40 hereafter), 90 g of lactose, 34 g of corn starch,20 g of crystalline cellulose and 1 g of magnesium stearate are mixed bymeans of a blender. The mixture is then pelletised by means of a tabletmaking machine to obtain tablets.

FORMULATION EXAMPLE 5

Eye drops

The following components are mixed:

    ______________________________________                                        (R)-N-[5-(1,2-dithiolan-3-yl)pentanoyl]methane-                                                          0.2 g                                                sulfonamide (the Compound of Example 40)                                      Disodium phosphate 0.716 g                                                    Sodium phosphate 0.728 g                                                      Sodium chloride 0.400 g                                                       Methyl p-hydroxybenzoate 0.026 g                                              Propyl p-hydroxybenzoate 0.014 g                                              Sterilised purified water q.s.                                                Sodium hydroxide q.s.                                                         Total 100 ml                                                                ______________________________________                                    

The pH of the mixture is adjusted to 7.0 and eye drops are prepared by aconventional method.

FORMULATION EXAMPLE 6

Eye drops

The following components are mixed:

    ______________________________________                                        (R)-N-[5-(1,2-dithiolan-3-yl)pentanoyl]methane-                                                          0.2 g                                                sulfonamide (the Compound of Example 40)                                      Disodium phosphate 0.716 g                                                    Sodium phosphate 0.728 g                                                      Sodium chloride 0.400 g                                                       Methyl p-hydroxybenzoate 0.026 g                                              Propyl p-hydroxybenzoate 0.014 g                                              Sterilised purified water q.s.                                                Ascorbic acid q.s.                                                            Sodium hydroxide q.s.                                                         Total 100 ml                                                                ______________________________________                                    

The pH of the mixture is adjusted to 7.0 and eye drops are prepared by aconventional method.

BIOLOGICAL ACTIVITY

The biological activity of the compounds of the present invention isillustrated by the following Test Examples.

TEST EXAMPLE 1 Measurement of Glutathione Reductase Activity

(a) Lens Tissue Culture

The test animals were 6 to 8 week old male SD rats (supplier: NipponSLC). The animals were sacrificed by suffocation by inhalation of carbondioxide. Both eyeballs of each test animal were then excised. Anincision was made in the sclera on the back of the eyeballs, and thenthe vitreous body and iris-ciliary body were removed, followed byremoval of the lens.

Each lens obtained in this manner was cultured by immersing it in 3 mlof the culture solution described below in a 6-well tissue culture plate(FALCON). Culturing was performed for 72 hours in a CO₂ incubatormaintained at 37° C. and 100% humidity in the presence of 5% CO₂ (inair).

Medium 199 (Gibco) containing penicillin (20 units/ml) and streptomycin(20 μg/ml) was used as the control culture solution.

The test culture solution contained the test compound added to theabove-mentioned culture solution. The cultured lenses were placed infrozen storage until the time of the test.

(b) Measurement of Glutathione Reductase Activity

After homogenising each frozen rat lens in 2 ml of distilled water, theresulting homogenate was separated by centrifugation (10,000 g, 20minutes) after which the resulting supernatant was used as the enzymesample.

400 μl of enzyme sample were added to 0.6 ml of phosphate buffercontaining 1 mM oxidized glutathione (GSSG) and 100 μM NADPH. After themixture had reacted at 25° C. for 6 minutes, the absorbance of thereaction mixture (at 340 nm: i.e. OD₃₄₀ nm) was measured. The difference(ΔOD₃₄₀ nm) between the OD₃₄₀ nm value before reaction and the OD₃₄₀ nmvalue after completion of the reaction was used as an indicator ofglutathione reductase activity.

The results for the compound of Example 2 are shown in the followingTable 4.

                  TABLE 4                                                         ______________________________________                                        Concentration of the compound of                                                Example 2 (μM) ΔOD.sub.340 nm /min/g protein                       ______________________________________                                        0                  3.10 ± 0.11                                               10 3.24 ± 0.10                                                             30 3.20 ± 0.09                                                             100 3.59 ± 0.05 (p < 0.05)                                                 300 3.70 ± 0.08 (p < 0.05)                                                 1000 4.16 ± 0.18 (p < 0.05)                                              ______________________________________                                    

The dithiolan derivatives of the present invention exhibited excellentglutathione reductase activity enhancing effects.

TEST EXAMPLE 2 Anti-cataract Test

The test animals were 6 week old male SD rats (supplier: Nippon SLC).The animals were sacrificed by suffocation by inhalation of carbondioxide. Both eyeballs of each test animal were then excised. Theexcised lenses were cultured at 37° C. for 24 hours in Medium 199(Gibco) containing 0.05 mg/ml of the test compound and 5 mM hydrogenperoxide. For the control test, excised lenses were cultured at 37° C.for 24 hours in normal culture liquid (Medium 199, Gibco) or Medium 199(Gibco) containing 5 mM hydrogen peroxide.

After culturing for 24 hours, the lenses were washed with physiologicalsaline. Surface moisture was removed by placing the lenses on a piece offilter paper, and then the lenses were placed on a slide glass afterwhich lens turbidity was scored under stereomicroscope from "-"(turbidity degree of the lens cultured in a normal culture medium) to"++++" (turbidity degree of the lens cultured in a medium containinghydrogen peroxide). The results are shown in Table 5.

                  TABLE 5                                                         ______________________________________                                        Compound of  Rat Lens turbidity in 5 mM                                         Example No. H.sub.2 O.sub.2, 24 hours                                       ______________________________________                                        1            ++                                                                 2 ++                                                                          7 +                                                                           8 ++                                                                          21 ++                                                                         43 ++                                                                         45 ++                                                                         46 +                                                                          50 +                                                                          52 +                                                                          55 +                                                                          56 ++                                                                         57 +                                                                          59 +                                                                          61 +                                                                          63 ++                                                                         70 ++                                                                         74 ++                                                                         79 ++                                                                         80 ++                                                                         86 ++                                                                         103 ++                                                                        106 ++                                                                        109 +                                                                         118 ++                                                                        123 ++                                                                        lipoic acid +++                                                               normal lens -                                                                 without drug +++                                                            ______________________________________                                    

As can be seen from the above results, the compounds of the presentinvention substantially improve the opacity of the lens.

EXAMPLES

The present invention is further illustrated by reference to thefollowing non-limiting Examples.

EXAMPLE 1 N-Acetyl-α-thioctamide (Compound No. 1-271) ##STR17##

A mixture of 0.76 g of D,L-α-thioctamide, 1.5 g of acetic anhydride and10 ml of pyridine was heated under reflux for 20 hours. The pyridine wasthen removed from the reaction mixture by distillation under reducedpressure, and water was added to the residue, which was then extractedwith ethyl acetate. The extraction solution was washed twice with waterand dried over anhydrous magnesium sulfate. 0.76 g of the crude productobtained by evaporating the solvent under reduced pressure was purifiedby silica gel column chromatography, using a 2:1 by volume mixture ofhexane and ethyl acetate as eluent, to obtain 0.45 g of3-(4-cyanobutyl)-1,2-dithiolan having [an Rf value of 0.84 (silica gelthin layer chromatography, using a 1:1 by volume mixture of hexane andethyl acetate as the developing solvent)] as a first component and 0.17g of the title compound, melting at 67° C. to 69° C. as a secondcomponent.

EXAMPLE 2 N-[5-(1,2-Dithiolan-3-yl)pentanoyl]methanesulfonamide(Compound No. 1-496) ##STR18## (a) 0.88 g of sodium hydride (as a 55% byweight dispersion in mineral oil) was washed with hexane, and 20 ml ofdimethylformamide and 1.96 g of methanesulfonamide were added to thedispersion at room temperature. The resulting mixture was subjected toultrasonic treatment for three hours and then left to stand at roomtemperature overnight, to give reaction mixture (A).

Separately, 2.06 g of D,L-α-lipoic acid were dissolved in 20 ml ofdimethylformamide, and 1.63 g of N,N'-carbonyldiimidazole were added tothe solution, whilst ice-cooling. The resulting mixture was then left tostand at room temperature overnight. At the end of this time, thereaction mixture was added dropwise to the above reaction mixture (A) atroom temperature, and the mixture was stirred for 7 hours. The reactionmixture was then heated at 130° C. for 3 hours, after which it was leftto cool, and then poured into ice-water. Diluted aqueous hydrochloricacid was added to the mixture to adjust the pH to 5, and the mixture wasextracted with ethyl acetate. The extraction solution was washed threetimes with a saturated aqueous solution of sodium chloride and thendried over anhydrous magnesium sulfate. The solvent was then removed bydistillation under reduced pressure, and the resulting residue waspurified by silica gel column chromatography, using a 4:1 by volumemixture of ethyl acetate and hexane and then ethyl acetate alone as theeluent, to obtain 0.12 g of the title compound, melting at 87° C. to 88°C.

(b) 25.0 g of D,L-α-lipoic acid were dissolved in 500 ml of anhydrousdimethylformamide, and 21.57 g of N,N'-carbonyldiimidazole were added tothe solution, whilst ice-cooling, after which the resulting mixture wasstirred at room temperature for 2 hours and 30 minutes. 12.65 g ofmethanesulfonamide and 5.80 g of sodium hydride (as a 55% w/w dispersionin mineral oil) were then added, whilst ice-cooling, to the reactionmixture, and the mixture was stirred at room temperature for 4 hours andthen left to stand at room temperature overnight. At the end of thistime, the solvent was removed from the reaction mixture by evaporationunder reduced pressure, and water was added to the residue, after whichit was extracted with ethyl acetate. The extraction solution was washedwith a saturated aqueous solution of sodium chloride and dried overanhydrous sodium sulfate, and then the solvent was removed byevaporation under reduced pressure. The residue thus obtained waspurified by silica gel column chromatography, using 1:1,2:1 and 3:1 byvolume mixtures of ethyl acetate and hexane as eluent, to obtain 19.85 gof the title compound, melting at 85° C. to 88° C.

EXAMPLE 3 N-[5-(1-Oxo-1,2-dithiolan-3-yl)pentanoyl]methanesulfonamide(Compound No. 2-496) ##STR19##

500 mg of N-[5-(1,2-dithiolan-3-yl)pentanoyl]methanesulfonamide(prepared as described in Example 2) were dissolved in 10 ml of acetone,and 0.44 ml of a 31% w/v aqueous solution of hydrogen peroxide was addedto the solution, whilst ice-cooling. The mixture was stirred and thenleft to stand at room temperature overnight. At the end of this time, afurther 0.2 ml of a 31% w/v aqueous solution of hydrogen peroxide wasadded to the reaction mixture, and then the mixture was stirred at roomtemperature for 30 minutes, and then stirred on an oil bath at 50° C.for 1 hour. The mixture was then left to stand at room temperature for 3days, after which it was stirred on an oil bath at 50° C. for 10 hours;it was then left to stand at room temperature overnight. The solvent wasthen removed from the reaction mixture by evaporation under reducedpressure, and water was added to the residue thus obtained, after whichit was extracted with ethyl acetate. The extraction solution was washedwith a saturated aqueous solution of sodium chloride and dried overanhydrous sodium sulfate, and then the solvent was removed byevaporation under reduced pressure. The residue thus obtained waspurified by reverse phase preparative silica gel column chromatography,using 1:3 and 2:3 by volume mixtures of acetonitrile and water as theeluent. The solvent was evaporated from the eluted fraction thusobtained under reduced pressure, and the fraction was lyophilised, toobtain 0.15 g of the title compound (diastereomer mixture) as acolorless oil having an Rf value of 0.43 (silica gel thin layerchromatography, using a 10:1 by volume mixture of ethyl acetate andmethanol as the developing solvent).

EXAMPLE 4 N-[5-(1,2-Dithiolan-3-yl)pentanoyl]methanesulfonamide sodiumsalt (Compound No. 1-496. sodium salt)

750 mg of N-[5-(1,2-dithiolan-3-yl)pentanoyl]methanesulfonamide(prepared as described in Example 2) were dissolved in 15 ml of ethylacetate, and 482 mg of sodium 2-ethylhexoate was added to the mixture atroom temperature. The mixture was stirred for 2 hours, after which itwas left to stand for 2 days at room temperature. The crystals whichprecipitated from the reaction mixture were collected by filtration, toobtain 550 mg of the title compound, melting at 202° C. to 204° C.

EXAMPLE 5 Ethyl 5-(1-oxo-1,2-dithiolan-3-yl)pentanoate and ethyl5-(2-oxo-1,2-dithiolan-3-yl)pentanoate (Compound No. 2-208 and CompoundNo. 3-208) ##STR20##

1.00 g of D,L-α-lipoic acid was dissolved in 20 ml of acetone, and 0.58g of a 31% w/v aqueous solution of hydrogen peroxide was added to thesolution on a dry ice-acetone bath. The mixture was stirred for 2 hours,and it was then left to stand at room temperature overnight. At the endof this time, the solvent was removed from the reaction mixture byevaporation under reduced pressure, and water was added to the residue,after which it was extracted with ethyl acetate. The extraction solutionwas washed with a saturated aqueous solution of sodium chloride anddried over anhydrous sodium sulfate, and then the solvent was removed byevaporation under reduced pressure. 16 ml of anhydrous ethanol and 4 mlof a 4 N solution of hydrogen chloride in ethyl acetate were added tothe residue thus obtained, and the mixture was stirred for 2 hours. Thesolvent was then removed from the reaction mixture by evaporation underreduced pressure, and the residue thus obtained was purified by silicagel column chromatography, using 1:2, 2:1 and 3:1 by volume mixtures ofethyl acetate and hexane as eluent, to obtain 0.26 g of ethyl5-(2-oxo-1,2-dithiolan-3-yl)pentanoate having an Rf value of 0.41(silica gel thin layer chromatography; using a 2:1 by volume mixture ofethyl acetate and hexane as the developing solvent) and 0.67 g of ethyl5-(1-oxo-1,2-dithiolan-3-yl)pentanoate having an Rf value of 0.29(silica gel thin layer chromatography; using a 2:1 by volume mixture ofethyl acetate and hexane as the developing solvent).

EXAMPLE 6 N-[4-(1,2-Dithiolan-3-yl)butyl]-N',N'-dimethylurea (CompoundNo. 1-815) ##STR21##

1.00 g of D,L-α-lipoic acid was dissolved in 20 ml of toluene, and 2.00ml of triethylamine and 1.25 ml of diphenylphosphoryl azide were addedto the resulting solution at room temperature, and then the mixture wasstirred on an oil bath at 80° C. for 2 hours. 0.47 g of dimethylaminehydrochloride was then added to the reaction mixture, and the mixturewas stirred at room temperature for 4 hours. At the end of this time,the solvent was removed from the reaction mixture by evaporation underreduced pressure, and 20 ml of anhydrous tetrahydrofuran and 0.52 ml ofa 50% v/v aqueous solution of dimethylamine were added to the residuethus obtained; the mixture was then left to stand at room temperatureovernight. The solvent was removed from the reaction mixture byevaporation under reduced pressure, and water was added to the residuethus obtained, after which it was extracted with ethyl acetate. Theextraction solution was washed with a saturated aqueous solution ofsodium chloride and dried over anhydrous sodium sulfate, and then thesolvent was removed by evaporation under reduced pressure. The residuethus obtained was purified by silica gel column chromatography, usingethyl acetate and then a 9:1 by volume mixture of ethyl acetate andmethanol as eluent. The solvent was evaporated from the fractionincluding the title compound under reduced pressure, and the residuethus obtained was dissolved in dioxane. The solution was lyophilised, toobtain 832 mg of the title compound, melting at 52° C. to 53° C.

EXAMPLE 7 N-[5-(1,2-Dithiolan-3-yl)pentanoyl]sulfamide (Compound No.1-539) ##STR22##

50 mg of D,L-α-lipoic acid were dissolved in 10 ml of anhydrousdimethylformamide, and 421 mg of N,N'-carbonyldiimidazole were added tothe solution, whilst ice-cooling, and then the mixture was stirred atroom temperature for 3 hours. 461 mg of sulfamide and 113 mg of sodiumhydride (as a 55% w/w dispersion in mineral oil) were then added to thereaction mixture, whilst ice-cooling, and the mixture was stirred for 4hours and then left to stand at room temperature overnight. At the endof this time, the solvent was removed from the reaction mixture byevaporation under reduced pressure, and water and 2 N aqueoushydrochloric acid were added to the residue thus obtained to adjust thepH to 5 to 6, after which it was extracted with ethyl acetate. Theextraction solution was washed with a saturated aqueous solution ofsodium chloride and dried over anhydrous sodium sulfate, and then thesolvent was removed by evaporation under reduced pressure. The residuethus 2:1 by volume mixture of ethyl acetate and hexane as the eluent,and the resulting fraction was then recrystallized from a 1:2 by volumemixture of ethanol, diisopropyl ether and hexane, to obtain 119 mg ofthe title compound, melting at 141° C. to 142° C.

EXAMPLE 8 N-[4-(1,2-Dithiolan-3-yl)butyl-N'-methylurea (Compound No.1-733) ##STR23##

1.00 g of D,L-α-lipoic acid was dissolved in 20 ml of toluene, and 2.00ml of triethylamine and 1.25 ml of diphenylphosphoryl azide were addedto the resulting solution at room temperature, after which the resultingmixture was stirred on an oil bath at 80° C. for 3 hours. The solventwas then removed from the reaction mixture by evaporation under reducedpressure, and 20 ml of tetrahydrofuran and 0.45 ml of a 40% v/v aqueoussolution of methylamine were added to the residue thus obtained, whilstice-cooling, and the mixture was stirred at room temperature for 3 hoursand then left to stand at room temperature overnight. The solvent wasremoved from the reaction mixture by evaporation under reduced pressure,and water was added to the residue thus obtained, after which it wasextracted with ethyl acetate. The extraction solution was washed with asaturated aqueous solution of sodium chloride and dried over anhydroussodium sulfate, and then the solvent was removed by evaporation underreduced pressure. The residue thus obtained was purified by silica gelcolumn chromatography, using ethyl acetate and then 20:1 and 10:1 byvolume mixtures of ethyl acetate and methanol as the eluent, to obtain425 mg of the title compound, melting at 89° C. to 90° C.

EXAMPLE 9 N-[4-(1,2-Dithiolan-3-yl)butyl]urea (Compound No. 1-693)##STR24##

1.00 g of D,L-α-lipoic acid was dissolved in 20 ml of toluene, and 0.80ml of triethylamine and 1.25 ml of diphenylphosphoryl azide were addedto the solution at room temperature, after which the resulting mixturewas stirred on an oil bath at 80° C. for 4 hours. The solvent was thenremoved from the reaction mixture by evaporation under reduced pressure,and 20 ml of tetrahydrofuran and 0.49 ml of 28% w/v aqueous ammonia wereadded to the residue thus obtained. The mixture was then stirred at roomtemperature for 4 hours, after which it was left to stand overnight. Thesolvent was then removed from the reaction mixture by evaporation underreduced pressure, and water and 2 N aqueous hydrochloric acid were addedto the mixture to adjust the pH to 2, after which it was extracted withethyl acetate. The extraction solution was washed with a saturatedaqueous solution of sodium chloride and dried over anhydrous sodiumsulfate, and then the solvent was removed by evaporation under reducedpressure. The residue thus obtained was purified by silica gel columnchromatography, using 10:1, 4:1 and 3:1 by volume mixtures of ethylacetate and methanol as eluent, to obtain 340 mg of the title compound,melting at 110° C. to 113° C.

EXAMPLE 10 N-[5-(1,2-Dithiolan-3-yl)pentanoyl]benzenesulfonamide(Compound No. 1-457) ##STR25##

1.00 g of D,L-α-lipoic acid was dissolved in 20 ml of anhydrousdimethylformamide, and 0.86 g of N,N'-carbonyldiimidazole was added tothe solution, whilst ice-cooling. The mixture was then stirred at roomtemperature for 2 hours and 30 minutes. 0.83 g of benzenesulfonamide and0.23 g of sodium hydride (as a 55% w/w dispersion in mineral oil) wereadded to the reaction mixture, whilst ice-cooling, and the mixture wasstirred for 2 hours. The solvent was then removed from the reactionmixture by evaporation under reduced pressure, and water and 2 N aqueoushydrochloric acid were added to the residue thus obtained to adjust thepH to 2, after which it was extracted with ethyl acetate. The extractionsolution was washed with a saturated aqueous solution of sodium chlorideand dried over anhydrous sodium sulfate, and then the solvent wasremoved by evaporation under reduced pressure. The residue thus obtainedwas purified by silica gel column chromatography, using 1:2, 1:1 and 2:1by volume mixtures of ethyl acetate and hexane as eluent, and then byreverse phase preparative silica gel column chromatography, using 3:7,1:1 and 7:3 by volume mixtures of acetonitrile and water as eluent. Thesolvent was evaporated under reduced pressure from the fractioncontaining the title compound, and the residue thus obtained wasdissolved in dioxane. The resulting solution was lyophilised, to obtain0.61 g of the title compound having an Rf value of 0.51 (silica gel thinlayer chromatography; using a 2:1 by volume mixture of ethyl acetate andhexane as the developing solvent).

EXAMPLE 11 N-[5-(1,2-Dithiolan-3-yl)pentanoyl]benzenesulfonamide sodiumsalt (Compound No. 1-457. sodium salt)

492 mg of N-[5-(1,2-dithiolan-3-yl)pentanoyl]benzenesulfonamide(prepared as described in Example 10) were dissolved in a mixture of 8ml of ethyl acetate and 1 ml of tetrahydrofuran, and 283 mg of sodium2-ethylhexoate were added to the mixture at room temperature. Theresulting mixture was stirred for 1 hour and 30 minutes, after which itwas left to stand for 2 days. The crystals which precipitated from thereaction mixture were collected by filtration to obtain 349 mg of thetitle compound, melting at 213° C. to 215° C.

EXAMPLE 12 N.sup.α -[5-(1,2-Dithiolan-3-yl)pentanoyl]-N^(im)-t-butoxycarbonylhistidine methyl ester (Compound No. 1-70) ##STR26##

500 mg of D,L-α-lipoic acid were dissolved in 10 ml of anhydrousdimethylformamide, and 422 mg of N,N'-carbonyldiimidazole were added tothe solution, whilst ice-cooling. The mixture was then stirred at roomtemperature for 2 hours. At the end of this time, 629 mg of L-histidinemethyl ester dihydrochloride salt and 0.70 ml of triethylamine wereadded to the reaction mixture, whilst ice-cooling, and the mixture wasstirred for 1 hour whilst ice-cooling, and then stirred at roomtemperature for a further 1 hour. The solvent was then removed from thereaction mixture by evaporation under reduced pressure, and water wasadded to the residue thus obtained, after which it was extracted withethyl acetate. The extraction solution was washed with a saturatedaqueous solution of sodium chloride and dried over anhydrous sodiumsulfate, and then the solvent was removed by evaporation under reducedpressure. The residue thus obtained was purified by silica gel columnchromatography, using ethyl acetate and then 20:1, 10:1 and 5:1 byvolume mixtures of ethyl acetate and methanol as eluent. The solvent wasevaporated from the fraction containing the product under reducedpressure, and then 5 ml of ethyl acetate were added to the residue thusobtained. 0.55 ml of di-t-butyl dicarbonate, 0.33 ml of triethylamineand a catalytic amount of N,N-dimethylaminopyridine were added to theresulting solution, and the mixture was stirred for 1 hour. The reactionmixture was then purified by silica gel column chromatography, using a2:1 by volume mixture of ethyl acetate and hexane and then ethyl acetatealone as eluent. The solvent was evaporated from the fraction containingthe title compound under reduced pressure and the residue thus obtainedwas dissolved in dioxane. The solution was lyophilised, to obtain 844 mgof the title compound having an Rf value of 0.41 (silica gel thin layerchromatography; using ethyl acetate as the developing solvent).

EXAMPLE 13 N.sup.α -[5-(1,2-Dithiolan-3-yl)pentanoyl] histidine(Compound No. 1-71) ##STR27##

764 mg of N.sup.α -[5-(1,2-dithiolan-3-yl)pentanoyl]-N^(im)-t-butoxycarbonylhistidine methyl ester (prepared as described inExample 12) were dissolved in 5 ml of methanol, and 5.1 ml of a 1 Naqueous solution of sodium hydroxide were added to the solution at roomtemperature, after which the resulting mixture was stirred for 2 hoursand 30 minutes. 2.60 ml of 2 N aqueous hydrochloric acid were then addedto the mixture, and the resulting mixture was stirred and then left tostand overnight. The solvent was removed from the reaction mixture byevaporation under reduced pressure and the residue thus obtained waspurified by reverse phase preparative silica gel column chromatography,using a 3:7 by volume mixture of acetonitrile and water as eluent, toobtain 0.51 g of a mixture of the title compound (77%), melting at 122°C. to 126° C., and sodium chloride (23%).

EXAMPLE 145-[5-(1,2-Dithiolan-3-yl)pentanoylamino]-1,2,4-dithiazole-3-thione(Compound No. 1-72) ##STR28##

500 mg of D,L-α-lipoic acid were dissolved in 10 ml of anhydrousdimethylformamide, and 428 mg of N,N'-carbonyldiimidazole were added tothe solution, whilst ice-cooling. The mixture was then stirred at roomtemperature for 3 hours, after which 391 mg of3-amino-1,2,4-dithiazole-5-thione were added to the reaction mixture,whilst ice-cooling, and the mixture was stirred for 1 hour and 30minutes. It was then left to stand at room temperature overnight. Thesolvent was removed from the reaction mixture by evaporation underreduced pressure, and water was added to the residue thus obtained,after which it was extracted with ethyl acetate. The extraction solutionwas washed with a saturated aqueous solution of sodium chloride anddried over anhydrous sodium sulfate, and then the solvent was removed byevaporation under reduced pressure. The residue thus obtained waspurified by silica gel column chromatography, using 1:2, 1:1 and 2:1 byvolume mixtures of ethyl acetate and hexane as eluent, and thenrecrystallized from a mixture of ethyl acetate and hexane, to obtain 372mg of the title compound, melting at 158° C. to 161° C.

EXAMPLE 15 4-(1,2-Dithiolan-3-yl)butylamine diphenylphosphate (CompoundNo. 1-1123 diphenylphosphate) ##STR29##

1.00 g of D,L-α-lipoic acid was dissolved in 20 ml of toluene, and 2.00ml of triethylamine and 1.25 ml of diphenylphosphoryl azide were addedto the solution at room temperature, after which the resulting mixturewas stirred on an oil bath at 80° C. for 2 hours and 30 minutes. Thesolvent was then removed from the reaction mixture by evaporation underreduced pressure, and 20 ml of tetrahydrofuran and 1.21 ml of a 40% w/vaqueous solution of O-methylhydroxylamine hydrochloride were added tothe residue thus obtained, whilst ice-cooling. 2 ml of methanol werethen added to the mixture, after which the mixture was stirred at roomtemperature for 6 hours and then left to stand overnight. The solventwas then removed from the reaction mixture by evaporation under reducedpressure, and water and 2 N aqueous hydrochloric acid were added to theresidue thus obtained to adjust the pH to 2, after which it wasextracted with ethyl acetate. The extraction solution was washed with asaturated aqueous solution of sodium chloride and dried over anhydroussodium sulfate, and then the solvent was removed by evaporation underreduced pressure. The residue thus obtained was purified by silica gelcolumn chromatography, using ethyl acetate and then a 3:1 by volumemixture of ethyl acetate and methanol as eluent, followed by reversephase preparative silica gel column chromatography (using 1:4 and 1:1 byvolume mixtures of acetonitrile and water as the eluent). The solventwas then removed from the fraction containing the title compound byevaporation under reduced pressure, and water was added to the residuethus obtained, after which it was extracted with ethyl acetate. Theextraction solution was washed with a saturated aqueous solution ofsodium chloride and dried over anhydrous sodium sulfate, and then thesolvent was removed by evaporation under reduced pressure. Ethyl acetatewas added to the residue thus obtained to recrystallise it, giving 116mg of the title compound, melting at 100° C. to 103° C.

EXAMPLE 16 N,N'-Bis[4-(1,2-dithiolan-3-yl)butyl]urea (Compound No.1-765) ##STR30##

3.0 g of D,L-α-lipoic acid were dissolved in 60 ml of toluene, and 2.40ml of triethylamine and 3.70 ml of diphenylphosphoryl azide were addedto the resulting solution at room temperature, after which the resultingmixture was stirred on an oil bath at 80° C. for 2 hours. The solventwas then removed from the reaction mixture by evaporation under reducedpressure, and 60 ml of t-butanol were added at room temperature to theresidue thus obtained. The mixture was then stirred and then left tostand for 5 days. At the end of this time, the solvent was removed fromthe reaction mixture by evaporation under reduced pressure, and theresidue thus obtained was purified by silica gel column chromatography,using 1:5 and 1:3 by volume mixtures of ethyl acetate and hexane aseluent. The solvent was then removed by evaporation under reducedpressure, and 5 ml of dioxane were added to the resulting residue. Thesolvent was then removed by evaporation under reduced pressure. 5 ml of2 N aqueous hydrochloric acid and 10 ml of methanol were added to theresidue thus obtained, and the mixture was stirred on an oil bath at 60°C. for 2 hours. The solvent was then removed from the reaction mixtureby evaporation under reduced pressure. Water was added to the residueand the mixture was neutralized with triethylamine, after which it wasextracted with ethyl acetate. The extraction solution was washed with asaturated aqueous solution of sodium chloride and dried over anhydroussodium sulfate. Ethyl acetate was removed from the extraction solutionby evaporation under reduced pressure, and the residue wasrecrystallized from ethyl acetate, to obtain 260 mg of a crude product.

160 mg of this crude product were purified by reverse phase preparativesilica gel column chromatography, using 2:3, 1:1, 3:2 and 7:3 by volumemixtures of acetonitrile and water as the eluent. The solvent was thenevaporated from the fraction containing the title compound under reducedpressure, to obtain 87 mg of the title compound, melting at 115° C. to116° C.

EXAMPLE 17 5-(1,2-Dithiolan-3-yl)pentanohydroxamic acid (Compound No.1-58) ##STR31##

500 mg of D,L-α-lipoic acid were dissolved in 10 ml of anhydrousdimethylformamide, and 428 mg of N,N'-carbonyldiimidazole were added tothe solution, whilst ice-cooling, and then the mixture was stirred atroom temperature for 2 hours and 30 minutes. 0.67 ml of triethylamineand 334 mg of hydroxylamine hydrochloride were then added to thereaction mixture, whilst ice-cooling, and the mixture was stirred atroom temperature for 2 hours and then left to stand overnight. At theend of this time, the solvent was removed from the reaction mixture byevaporation under reduced pressure, and water and 2 N aqueoushydrochloric acid were added to the residue thus obtained to adjust thepH to 6 to 7, after which it was extracted with ethyl acetate. Theextraction solution was washed with a saturated aqueous solution ofsodium chloride and dried over anhydrous sodium sulfate, and then thesolvent was removed by evaporation under reduced pressure. The residuethus obtained was purified by silica gel column chromatography, using a4:1 by volume mixture of ethyl acetate and hexane, followed by a 20:1 byvolume mixture of ethyl acetate and methanol, as eluent, and then byreverse phase preparative silica gel column chromatography, using 3:7and 1:1 by volume mixtures of acetonitrile and water as eluent. Theproduct thus obtained was lyophilised, to obtain 0.38 g of the titlecompound, melting at 63° C. to 64° C.

EXAMPLE 18N-[4-(1,2-Dithiolan-3-yl)butyl-N'-[1-methoxycarbonyl-2-(4-methoxybenzylthio)ethyl]urea(Compound No. 1-766) ##STR32##

300 mg of D,L-α-lipoic acid were dissolved in 6 ml of toluene, and 0.24ml of triethylamine and 0.37 ml of diphenylphosphoryl azide were addedto the solution at room temperature. The mixture was then stirred on anoil bath at 80° C. for 2 hours. At the end of this time, a solution of434 mg of S-(4-methoxybenzyl)-L-cysteine methyl ester in 3 ml ofanhydrous tetrahydrofuran was added to the reaction mixture, whilstice-cooling, and the mixture was stirred at room temperature for 3 hoursand then left to stand overnight. The solvent was then removed from thereaction mixture by evaporation under reduced pressure, and the mixturewas recrystallized from ethyl acetate, to obtain 434 mg of the titlecompound, melting at 105° C. to 107° C.

EXAMPLE 19 Hydrazine-N,N'-dicarboxylic acidbis[4-(1,2-dithiolan-3-yl)butylamide] (Compound No. 1-936) ##STR33##

1.00 g of D,L-α-lipoic acid was dissolved in 20 ml of toluene, and 2.00ml or triethylamine and 1.25 ml of diphenylphosphoryl azide were addedto the resulting solution. The mixture was then stirred on an oil bathat 70° C. for 2 hours. 0.19 ml of anhydrous hydrazine was then added tothe reaction mixture, whilst ice-cooling, and the mixture was stirred atroom temperature for 2 hours. The solvent was then removed from thereaction mixture by evaporation under reduced pressure, and the residuethus obtained was washed with water and with ethyl acetate. Theinsolubles were then collected by filtration. The insolubles thusobtained were washed with a 5:2:1 by volume mixture of methanol,tetrahydrofuran and dimethylformamide, to obtain 401 mg of the titlecompound, melting at 205° C. to 207° C.

EXAMPLE 20 N-[5-(1,2-Dithiolan-3-yl)pentanoyl]ethanesulfonamide(Compound No. 1-497) ##STR34##

500 mg of D,L-α-lipoic acid were dissolved in 10 ml of anhydrousdimethylformamide, and 428 mg of N,N'-carbonyldiimidazole were added tothe solution, whilst ice-cooling. The mixture was then stirred at roomtemperature for 1 hour. At the end of this time, a solution of 284 mg ofethanesulfonamide in 3 ml of dimethylformamide and 113 mg of sodiumhydride (as a 55% w/w dispersion in mineral oil) were added to thereaction mixture, whilst ice-cooling, and the mixture was stirred atroom temperature for 1 hour and then left to stand for 3 days. Thesolvent was then removed from the reaction mixture by evaporation underreduced pressure, and water and 2 N aqueous hydrochloric acid were addedto the residue thus obtained to adjust the pH to 2, after which it wasextracted with ethyl acetate. The extraction solution was washed with asaturated aqueous solution of sodium chloride and dried over anhydroussodium sulfate, and then the solvent was removed by evaporation underreduced pressure. The residue thus obtained was purified by silica gelcolumn chromatography, using 1:1 and 2:1 by volume mixtures of ethylacetate and hexane as eluent, followed by reverse phase preparativesilica gel column chromatography, using 3:7, 2:3 and 1:1 by volumemixtures of acetonitrile and water as eluent. The solvent was thenremoved from the eluted fraction thus obtained by evaporation underreduced pressure, and the residue thus obtained was dissolved indioxane. The solution was lyophilised, to obtain 30 mg of the titlecompound, melting at 98° C. to 100° C.

EXAMPLE 21 1,1-Dimethyl-4-[4-(1,2-dithiolan-3-yl)butyl]semicarbazide(Compound No. 1-861) ##STR35##

1.00 g of D,L-α-lipoic acid was dissolved in 10 ml of toluene, and 0.80ml of triethylamine and 1.25 ml of diphenylphosphoryl azide were addedto the resulting solution, after which the resulting mixture was stirredon an oil bath at 80° C. for 1 hour. 0.55 ml of 1,1-dimethylhydrazinewas then added to the mixture, whilst ice-cooling, and the mixture wasstirred at room temperature for 1 hour and then left to stand overnight.At the end of this time, the solvent was removed from the reactionmixture by evaporation under reduced pressure, and water was added tothe residue thus obtained, after which it was extracted with ethylacetate. The extraction solution was washed with a saturated aqueoussolution of sodium chloride and dried over anhydrous sodium sulfate, andthen the solvent was removed by evaporation under reduced pressure. Theresidue thus obtained was purified by silica gel column chromatography,using a 3:1 by volume mixture of ethyl acetate and hexane and then a10:1 by volume mixture of ethyl acetate and methanol as eluent, followedby reverse phase preparative silica gel column chromatography, using7:13 and 2:3 by volume mixtures of acetonitrile and water as eluent. Theeluted fraction thus obtained was lyophilised, to obtain 0.99 g of thetitle compound, melting at 60° C. to 61° C.

EXAMPLE 22 Morpholine-4- carboxylic acid 4-(1,2-dithoilan-3-yl)butylamide (Compound No. 1-1142) ##STR36##

500 mg of D,L-α-lipoic acid were dissolved in 10 ml of toluene, and 0.36ml of triethylamine and 0.56 ml of diphenylphosphoryl azide were addedto the resulting solution, after which the resulting mixture was stirredon an oil bath at 80° C. for 1 hour and 30 minutes. 0.23 ml ofmorpholine was then added to the mixture, whilst ice-cooling, and themixture was stirred at room temperature for 2 hours and then left tostand overnight. The solvent was removed from the reaction mixture byevaporation under reduced pressure, and water was added to the residuethus obtained, after which it was extracted with ethyl acetate. Theextraction solution was washed with a saturated aqueous solution ofsodium chloride and dried over anhydrous sodium sulfate, and then thesolvent was removed by evaporation under reduced pressure. The residuethus obtained was purified by silica gel column chromaatography, usingethyl acetate and then a 10:1 by volume mixture of ethyl acetate andmethanol as eluent, followed by reverse phase preparative silica gelcolumn chromatography, using 3:7 and 2:3 by volume mixtures ofacetonitrile and water as eluent. The solvent was evaporated from theeluted fraction thus obtained under reduced pressure, and water wasadded to the residue, after which it was extracted with ethyl acetate.The extraction solution was washed with a saturated aqueous solution ofsodium chloride and dried over anhydrous sodium sulfate, and then thesolvent was removed by evaporation under reduced pressure, The residuethus obtained was dissolved in dioxane, and the solution waslyophilised, to obtain 0.51 g of the title compound, melting at 74° C.to 77° C.

EXAMPLE 23 N-Hydroxy-N'-[4-(1,2-dithiolan-3-yl)butyl]urea (Compound No.1-750) ##STR37##

500 mg of D,L-α-lipoic acid were dissolved in 10 ml of toluene, and 0.69ml of triethylamine and 0.56 ml of diphenylphosphoryl azide were addedto the resulting solution, after which the resulting mixture was stirredon an oil bath at 80° C. for 2 hours. The solvent was then removed fromthe removed from the reaction mixture by evaporation under reducedpressure, and 10 ml of anhydrous tetrahydrofuran and 181 mg ofhydroxylamine hydrochloride were added to the residue thus obtained on abath containing ice and an aqueous solution of sodium chloride. Themixture was stirred for 2 hours at the bath temperature, and thenstirred at room temperature for 3 hours, after which it was left tostand for 3 days. The solvent was then removed from the reaction mixtureby evaporation under reduced pressure, and water was added to theresidue thus obtained, after which it was extracted with ethyl acetate.The extraction solution was washed with a saturated aqueous solution ofsodium chloride and dried over anhydrous sodium sulfate, and then thesolvent was removed by evaporation under reduced pressure, The residuethus obtained was subjected to silica gel column chromatography, elutedfirst with a 2:1 by volume mixture of ethyl acetate and hexane, thenwith ethyl acetate alone, and finally with a 10:1 by volume mixture ofethyl acetate and methanol. The solvent was removed from the elutedfraction thus obtained by evaporation under reduced pressure, and theprecipitated powder was washed with a mixture of dimethylformamide,tetrahydrofuran, methanol and ethyl acetate and subjected to reversephase preparative silica gel column chromatography, using 3:7 and 1:1 byvolume mixtures of acetonitrile and water as eluent. The eluted fractionthus obtained was concentrated by evaporation under reduced pressure,and the crystals which precipitated were collected by filtration, toobtain 85 mg of the title compound, melting at 100° C. to 101° C.

EXAMPLE 24 2-[5-(1,2-Dithiolan-3-yl)pentanoylamino]ethanesulfonic acidimidazole salt (Compound No. 1-57 imidazole salt) ##STR38##

500 mg of D,L-α-lipoic acid were dissolved in 10 ml of anhydrousdimethylformamide, and 428 mg of N,N'-carbonyldiimidazole were added tothe resulting solution, whilst ice-cooling, and then the mixture wasstirred at room temperature for 4 hours. At the end of this time, 0.50ml of triethylamine and 450 mg of 2-aminoethanesulfonic acid were addedto the reaction mixture, whilst ice-cooling, and the mixture was stirredat room temperature of 4 hours and 30 minutes and then left to stand of2 days. After this time, the reaction mixture was stirred on an oil bathat 50° C. for 6 hours and then stirred on an oil bath at 70° C. for 1hour. It was then left to stand at room temperature overnight. Thereaction mixture was then stirred on an oil bath at 70° C. for 2 hoursand the solvent was removed from the reaction mixture by evaporationunder reduced pressure, The residue thus obtained was washed with ethylacetate and subjected to reverse phase preparative silica gel columnchromatography, using a 1:9 by volume mixture of acetonitrile and wateras eluent. The eluted fraction thus obtained was lyophilised, to obtain268 mg of the title compound, melting at 96° C. to 99° C.

EXAMPLE 25 N.sup.β -[5-(1,2-Dithiolan-3-yl)pentanoyl]histamine (CompoundNo. 1-75) ##STR39##

500 mg of D,L-α-lipoic acid were dissolved in 10 ml of anhydrousdimethylformamide, and 422 mg of N,N'-carbonyldiimidazole were added tothe resulting solution, whilst ice-cooling. The mixture was then stirredat room temperature for 2 hours and 30 minutes. 0.73 ml of triethylamineand 479 mg of histamine dihydrochloride were then added to the reactionmixture at room temperature, and the mixture was stirred for 4 hours and30 minutes. At the end of this time, the solvent was removed from thereaction mixture by evaporation under reduced pressure, and water wasadded to the residue thus obtained, after which it was extracted withethyl acetate. The extraction solution was washed with a saturatedaqueous solution of sodium chloride and dried over anhydrous sodiumsulfate, and then the solvent was removed by evaporation under reducedpressure. The residue thus obtained was purified by silica gel columnchromatography, using 1:0, 5:1 and 3:1 by volume mixtures of ethylacetate and ethanol as eluent. It was then recrystallized from a 1:2 byvolume mixture of ethyl acetate and diisopropyl ether, to obtain 270 mgof the title compound, melting at 108° C. to 110° C.

EXAMPLE 26 N,N'-Bis[4-(1,2-dithiolan-3-yl)butylcarbamoyl]sulfamide(Compound No. 1-2614) ##STR40##

500 mg of D,L-α-lipoic acid were dissolved in 10 ml of toluene, and then0.36 ml of triethylamine and 0.56 ml of diphenylphosphoryl azide wereadded to the mixture, after which the resulting mixture was stirred onan oil bath at 80° C. for 2 hours. The solvent was then removed from thereaction mixture by evaporation under reduced pressure, and 6 ml ofanhydrous dimethylformamide were added to the residue thus obtained, togive a dimethylformamide solution.

Separately, 113 mg of sodium hydride (as a 55% w/w dispersion in mineraloil) were dispersed in 4 ml of dimethylformamide, and 252 mg ofsulfamide were added to the suspension, whilst ice-cooling, after whichthe resulting mixture was stirred at room temperature for 2 hours. Theabove dimethylformamide solution was then added to the reaction mixtureon a bath containing ice and an aqueous solution of sodium chloride, andthe mixture was stirred at the same temperature of 1 hour and 30minutes. The reaction mixture was then stirred at room temperature of 4hours, after which it was left to stand at room temperature overnight.The solvent was the removed from the reaction mixture by evaporationunder reduced pressure, and water was added to the residue thusobtained, after which it was neutralized by the addition of 2 N aqueoushydrochloric acid. The crystals which precipitated were washed withethyl acetate, with water and with ethanol, to obtain 223 mg of thetitle compound, melting at 153° C. to 156° C.

EXAMPLE 27 N.sup.β,N^(im)-Bis[4-(1,2-dithiolan-3-yl)butylcarbamoyl]histamine ##STR41##

500 mg of D,L-α-lipoic acid were dissolved in 10 ml of toluene, and then0.36 ml of triethylamine and 0.56 ml of diphenylphosphoryl azide wereadded to the solution, after which the resulting mixture was stirred onan oil bath at 80° C. for 1 hour and 30 minutes. The solvent was thenremoved form the reaction mixture by evaporation under reduced pressure,and 5 ml of anhydrous tetrahydrofuran were added to the residue thusobtained, to give a tetrahydrofuran solution.

Separately, 479 mg of histamine dihydrochloride were dissolved in 2 mlof anhydrous dimethylformamide, and then 0.72 ml of triethylamine wasadded to the solution, after which the resulting mixture was stirred atroom temperature for 1 hour and 30 minutes. 5 ml of anhydroustetrahydrofuran were then added to the reaction mixture, and then theabove anhydrous tetrahydrofuran solution was added thereto, whilstice-cooling. The mixture was stirred at room temperature for 3 hours andthen left to stand overnight. At the end of this time, the solvent wasremoved from the reaction mixture by evaporation under reduced pressure,and water was added to the residue thus obtained, after which it wasextracted with ethyl acetate. The extraction solution was washed with asaturated aqueous solution of sodium chloride and dried over anhydroussodium sulfate, and then the solvent was removed by evaporation underreduced pressure, The residue thus obtained was subjected to silica gelcolumn chromatography, using 1:0, 5:1 and 3:1 by volume mixtures ofmethanol as the eluent, after which ti was subjected to reverse phasepreparative silica gel column chromatography, using 1:4, 3:7, 2:3 and1:1 by volume mixtures of acetonitrile and water as eluent. The solventwas evaporated under reduced pressure from the fraction containing thetitle compound, and water was added to the residue thus obtained, afterwhich it was extracted with ethyl acetate. The extraction solution waswashed with a saturated aqueous solution of sodium chloride and driedover anhydrous sodium sulfate. The solvent was removed form theextraction solution by evaporation under reduced pressure, and theresidue thus obtained was dissolved in dioxane and lyophilised, toobtain 52 mg of the title compound, melting at 115° C. to 117° C.

EXAMPLE 28 N-[4-(1,2-Dithiolan-3-yl)butyl]-N'-methanesulfonylurea(Compound No. 1-1069) ##STR42##

500 mg of D,L-α-lipoic acid were dissolved in 10 ml of toluene, and then0.36 ml of triethylamine and 0.56 ml of diphenylphosphoryl azide wereadded to the solution, after which the resulting mixture was stirred onan oil bath at 80° C. for 2 hours. The solvent was removed from thereaction mixture by evaporation under reduced pressure, and 5 ml ofanhydrous dimethylformamide were added to the residue thus obtained, togive a dimethylformamide solution.

Separately, 247 mg of methanesulfonamide were dissolved in 5 ml ofanhydrous dimethylformamide, and then 113 mg of sodium hydride (as a 55%w/w dispersion in mineral oil) were added to the solution, after whichthe resulting mixture was stirred at room temperature for 2 hours. Theabove anhydrous dimethylformamide solution was then added to thereaction mixture, whilst ice-cooling, and the mixture was stirred atroom temperature for 3 hours and then left to stand at room temperatureof 3 days. The solvent was removed from the reaction mixture byevaporation under reduced pressure. Water was added to the residue thusobtained, and the mixture was neutralized by the addition of 2 N aqueoushydrochloric acid, after which it was extracted with ethyl acetate. Theextraction solution was washed with a saturated aqueous solution ofsodium chloride and dried over anhydrous sodium sulfate. The solvent wasremoved from the extraction solution by evaporation under reducedpressure. The residue thus obtained was purified by silica gel columnchromatography, using ethyl acetate as eluent, and the active fractionwas then recrystallized from ethyl acetate, to obtain 302 mg of thetitle compound, melting at 125° C. to 127° C.

EXAMPLE 29 4-[4-(1,2-Dithoilan-3-yl)butyl]simicarbazidediphenylphosphate (Compound No. 1-858 diphenylphosphate) ##STR43##

500 mg of D,L-α-lipoic acid were dissolved in 10 ml of toluene, and then0.36 ml of triethylamine and 0.56 ml of diphenylphosphoryl azide wereadded to the solution, after which the resulting mixture was stirred onan oil bath at 80° C. for 1 hour and 30 minutes. The solvent was removedfrom the reaction mixture by evaporation under reduced pressure, and 3.5ml of anhydrous tetrahydrofuran were added to the residue thus obtained,The solution was added to 0.75 mg of hydrazine and then 2 ml ofanhydrous dimethylformamide were added thereto. The mixture was stirredat room temperature for 5 hours and then left to stand overnight. At theend of this time, the solvent was removed from the reaction mixture byevaporation under reduced pressure, and a saturated aqueous solution ofsodium chloride was added to the residue thus obtained, after which itwas extracted with ethyl acetate. The extraction solution was washedwith a saturated aqueous solution of sodium chloride and dried overanhydrous sodium sulfate. The solvent was removed from the extractionsolution by evaporation under reduced pressure. The residue thusobtained was purified by silica gel column chromatography, using 1:0,10:1 and 5:1 by volume mixtures of ethyl acetate and methanol as eluent,after which it was recrystallized form a 1:1 by volume mixture of ethylacetate and diisopropyl ether, to obtain 125 mg of the title compound,melting at 134° C. to 139° C.

EXAMPLE 30 N-[4-(1,2-Dithiolan-3-yl)butyl]-N'-aminosulfonylurea(Compound No. 1-1112) ##STR44##

500 mg of D,L-α-lipoic acid were dissolved on 10 ml of toluene, and then0.36 ml of triethylamine and 0.56 ml of diphenylphosphoryl azide wereadded to the solution, after which the resulting mixture was stirred onan oil bath at 70° C. for 2 hours. The solvent was then removed from thereaction mixture by evaporation under reduced pressure, and 5 ml ofanhydrous dimethylformamide were added to the residue thus obtained, togive a dimethylformamide solution.

Separately, 1.15 g of sulfamide were dissolved in 10 ml of anhydrousdimethylformamide, and then 524 mg of sodium hydride (as a 55% w/wdispersion in mineral oil) were added to the solution, whilstice-cooling, after which the resulting mixture was stirred at roomtemperature for 1 hour and 30 minutes. The above dimethylformamidesolution was then added to the reaction mixture, whilst ice-cooling, andthe mixture was stirred at room temperature for 4 hours and then left tostand for 2 days. At the end of this time, the solvent was removed fromthe reaction mixture by evaporation under reduced pressure, and waterwas added to the residue thus obtained. The mixture was neutralized bythe addition of 2 N aqueous hydrochloric acid, after which it wasextracted with ethyl acetate. The extraction solution was washed with asaturated aqueous solution of sodium chloride and dried over anhydroussodium sulfate. The solvent was removed from the extraction solution byevaporation under reduced pressure, The residue thus obtained waspurified by silica gel column chromatography, using 1:1, 2:1 and 4:1 byvolume mixtures of ethyl acetate and hexane as eluent. It was thenrecrystallized from ethanol, to obtain 126 mg of the title compound,melting at 123° C. to 125° C.

EXAMPLE 31 Methyl N-[4-(1,2-Dithiolan-3-yl)butyl]carbamate (Compound No.1-676) ##STR45##

500 mg of D,L-α-lipoic acid were dissolved in 10 ml of toluene, and then0.36 ml of triethylamine and 0.56 ml of diphenylphosphoryl azide wereadded to the solution, after which the resulting mixture was stirred onan oil bath at 80° C. for 1 hour. The solvent was then removed from thereaction mixture by evaporation under reduced pressure, and 10 ml ofanhydrous methanol were added to the residue thus obtained. The mixturewas stirred at room temperature of 6 hours and then left to standovernight. At the end of this time, the solvent was removed from thereaction mixture by evaporation under reduced pressure, and water wasadded to the residue thus obtained, after which it was extracted withethyl acetate. The extraction solution was washed with a saturatedaqueous solution of sodium chloride and dried over anhydrous sodiumsulfate. The solvent was removed from the extraction solution byevaporation under reduced pressure. The residue thus obtained waspurified by silica gel column chromatography, using 1:4 and 1:2 byvolume mixtures of ethyl acetate and hexane as eluent, after which itwas subject to reverse phase column chromatography, using 1:4, 3:7, 2:3and 1:1 by volume mixtures of acetonitrile and water as eluent. Thesolvent was evaporated under reduced pressure from the fractioncontaining the title compound, and water was added to the residue thusobtained, after which it was extracted with ethyl acetate. Theextraction solution was washed with a saturated aqueous solution ofsodium chloride and dried over anhydrous sodium sulfate. The solvent wasremoved from the extraction solution by evaporation under reducedpressure, and the residue was dissolved in dioxane and lyophilised, toobtain 324 mg of the title compound, melting at 31° C. to 32° C.

EXAMPLE 32 N-[2-(5-Methoxy-1H-indol-3-yl)ethyl]lipoamide (Compound No.1-80) ##STR46##

500 mg of D,L-α-lipoic acid were dissolved in 10 ml of anhydrousdimethylformamide, and 422 mg of N,N'-carbonyldiimidazole were added tothe solution, whilst ice-cooling. The mixture was then stirred at roomtemperature of 3 hours and 30 minutes. At the end of this time, 495 mgof 5-methoxytryptamine were added to the reaction mixture, whilstice-cooling, and the mixture was stirred at room temperature for 3 hoursand then left to stand at room temperature overnight. The solvent wasremoved from the reaction mixture by evaporation under reduced pressure,and water was added to the residue thus obtained. The residue wasextracted with ethyl acetate and then dried over anhydrous sodiumsulfate. The solvent was removed form the extraction solution byevaporation under reduced pressure. The residue thus obtained waspurified by silica gel column chromatography, using 2:1, 4:1 and 1:0 byvolume mixtures of ethyl acetate and hexane as eluent, to obtain 515 mgof the title compound as a yellow oil having an Rf value of 0.26 (silicagel thin layer chromatography; using a 2:1 by volume mixture of ethylacetate and hexane as the developing solvent).

EXAMPLE 33N-[4-(1,2-Dithiolan-3-yl)butyl]-N'-[2-(5-methoxy-1H-indol-3-yl)ethyl]urea(Compound No. 1-772) ##STR47##

500 mg of D,L-α-lipoic acid were dissolved in 10 ml of toluene, and then0.36 ml of triethylamine and 0.56 ml of diphenylphosphoryl azide wereadded to the solution, after which the resulting mixture was stirred onan oil bath at 80° C. for 1 hour The solvent was then removed from thereaction mixture by evaporation under reduced pressure, and 5 ml ofanhydrous tetrahydrofuran were added to the residue thus obtained, togive a tetrahydrofuran solution.

Separately, 1.37 mg of 5-methoxytryptamine were dissolved in a mixtureof 10 ml of anhydrous tetrahydrofuran and 4 ml of anhydrousdimethylformamide, and the resulting solution was added to the aboveanhydrous tetrahydrofuran solution. whilst ice-cooling. The mixture wasstirred, whilst ice-cooling, for 1 hour and then at room temperature for4 hours, after which it was left to stand at room temperature overnight.The solvent was then removed from the reaction mixture by evaporationunder reduced pressure, and a saturated aqueous solution of sodiumchloride was added to the residue thus obtained, after which it wasextracted with ethyl acetate. The extraction solution was washed with asaturated aqueous solution of sodium chloride and then dried overanhydrous sodium sulfate. The solvent was removed from the extractionsolution by evaporation under reduced pressure. The residue thusobtained was purified by silica gel column chromatography, using 3:1 and1:0 by volume mixtures of ethyl acetate and hexane and then a 10:1 byvolume mixture of ethyl acetate and methanol as eluent, after which itwas recrystallized from ethyl acetate, to obtain 674 mg of the titlecompound, melting at 100° C. to 101° C.

EXAMPLE 34 N-[4-(1,2-Dithiolan-3-yl)butyl]pyrrolidine-1-carboxamide(Compound No. 1-1139) ##STR48##

500 mg of D,L-α- lipoic acid were dissolved in 10 ml of anhydroustoluene, and then 0.56 ml of diphenylphosphoryl azide was added to thesolution, after which the resulting mixture was stirred on an oil bathat 80° C. for 1 hour and 30 minutes. 0.22 ml of pyrrolidine was thenadded to the reaction mixture, whilst ice-cooling, and the mixture wasstirred at room temperature for 1 hour and then let to stand at roomtemperature overnight. At the end of this time, the solvent was removedfrom the reaction mixture by evaporation under reduced pressure, andwater was added to the residue thus obtained, after which it wasextracted with ethyl acetate. The extraction solution was washed with asaturated aqueous solution of sodium chloride and then dried overanhydrous sodium sulfate. The solvent was removed from the extractionsolution by evaporation under reduced pressure. The residue thusobtained was purified by silica gel column chromatography, using 1:0 and10:1 by volume mixtures of ethyl acetate and methanol as eluent, afterwhich it was recrystallized form a 1:1:1 by volume mixture of ethylacetate, methanol and acetonitrile, to obtain 231 mg of the titlecompound, melting at 91° C. to 93° C.

EXAMPLE 35 1-[5-(1,2-Dithiolan-3-yl)pentanoyl]pyrrolidine (Compound No.1-1129) ##STR49##

500 mg of D,L-α-lipoic acid were dissolved in 10 ml of anhydrousdimethylformamide, and then 422 mg of N,N'-carbonyldiimidazole wereadded to the solution. The resulting mixture was then stirred at roomtemperature for 1 hour and 30 minutes. 0.22 ml of pyrrolidine was addedto the reaction mixture, whilst ice-cooling, and the mixture was stirredat room temperature for 2 hours. At the end of this time, the solventwas removed from the reaction mixture by evaporation under reducedpressure, and water was added to the residue thus obtained, after whichit was extracted with ethyl acetate. The extraction solution was washedwith a saturated aqueous solution of sodium chloride and dried overanhydrous sodium sulfate. The solvent was removed from the extractionsolution by evaporation under reduced pressure. The residue thusobtained was purified by silica gel column chromatography, using 2:1,3:1 and 1:0 by volume mixtures of ethyl acetate and hexane as eluent,after which it was dissolved in dioxane and lyophilised, to obtain 364mg of the title compound as a yellow oil having an Rf value of 0.15(silica gel thin layer chromatography, using ethyl acetate as thedeveloping solvent).

EXAMPLE 36 N-[4-(1,2-Dithiolan-3yl)butyl]piperidine-1-carboxamide(Compound No. 1-1140) ##STR50##

500 mg of D,L-α-lipoic acid were dissolved in 10 ml of anhydroustoluene, and then 0.36 ml of triethylamine and 0.56 ofdiphenylphosphoryl azide were added to the solution, after which theresulting mixture was stirred on an oil bath at 80° C. for 1 hour. 0.26ml of piperidine was then added to the reaction mixture, whilstice-cooling, and the mixture was left to stand at room temperatureovernight. At the end of this time, the solvent was removed from thereaction mixture by evaporation under reduced pressure, and water wasadded to the residue thus obtained, after which it was extracted withethyl acetate. The extraction solution was washed with a saturatedaqueous solution of sodium chloride and then dried over anhydrous sodiumsulfate. The solvent was then removed from the extraction solution byevaporation under reduced pressure, The residue thus obtained waspurified by silica gel column chromatography, using 2:1, 4:1 and 1:0 byvolume mixtures of ethyl acetate and hexane as eluent. It was thenrecrystallized from a 1:1 by volume mixture of ethyl acetate andmethanol, to obtain 252 mg of the title compound, melting at 90° C. to91° C.

EXAMPLE 37 1-[5-(1,2-Dithiolan-3-yl)pentanoyl]piperidine (Compound No.1-1130) ##STR51##

500 mg of D,L-α-lipoic acid were dissolved in 10 ml of anhydrousdimethylformamide, and then 422 mg of N,N'-carbonyldiimidazole wereadded to the solution. The mixture was then stirred at room temperaturefor 3 hours. At the end of this time, 0.26 ml of piperidine was added tothe reaction mixture, and the mixture was stirred at room temperaturefor 4 hours and then left to stand overnight. The solvent was thenremoved from the reaction mixture by evaporation under reduced pressure,and water was added to the residue thus obtained, after which it wasextracted with ethyl acetate. The extraction solution was washed with asaturated aqueous solution of sodium chloride and dried over anhydroussodium sulfate. The solvent was removed from the extraction solution byevaporation under reduced pressure. The residue thus obtained waspurified by silica gel column chromatography, using 3:2 and 3:1 byvolume mixtures of ethyl acetate and hexane as eluent. It was thendissolved in dioxane and lyophilised, to obtain 381 mg of the titlecompound as a yellow oil having an Rf value of 0.30 (silica gel thinlayer chromatography, using a 3:2by volume mixture of ethyl acetate andhexane as the developing solvent).

EXAMPLE 38 N-[4-(1,2-Dithiolan-3-yl)butyl]thiomorpholine-4-carboxamide(Compound No. 1-1143) ##STR52##

500 mg of D,L-α-lipoic acid was dissolved in 10 ml of anhydrous toluene,and then 0.36 ml of triethylamine and 0.56 of diphenylphosphoryl azidewere added to the solution after which the resulting mixture was stirredon an oil bath at 80° C. for 1 hour. 0.25 ml of thiomorpholine was thenadded to the reaction mixture at room temperature, and the mixture wasstirred for 5 hours and then left to stand for 2 days. At the end ofthis time, the solvent was removed from the reaction mixture byevaporation under reduced pressure, and water was added to the residuethus obtained, after which it was extracted with ethyl acetate. Theextraction solution was washed with a saturated aqueous solution ofsodium chloride and then dried over anhydrous sodium sulfate. Thesolvent was removed from the extraction solution by evaporation underreduced pressure, The residue thus obtained was purified by silica gelcolumn chromatography, using 3:2, 3:1 and 1:0 by volume mixtures ofethyl acetate and hexane as eluent. It was then dissolved in dioxane andlyophilised, to obtain 583 mg of the title compound, melting at 80° C.to 81° C.

EXAMPLE 39 (S)-N-[5-(1,2-Dithiolan-3-yl)pentanoyl]methanesulfonamide(Compound No. 1-496) ##STR53##

300 mg of (S)-α-lipoic acid were dissolved in 6 ml of anhydrousdimethylformamide, and 276 mg of N,N'-carbonyldiimidazole and 1 ml ofanhydrous dimethylformamide were added to the solution, whilstice-cooling. The mixture was then stirred at room temperature for 1 hourand 30 minutes. At the end of this time, 162 mg of methanesulfonamideand 74 mg of sodium hydride (as a 55% w/w dispersion in mineral oil)were added to the reaction mixture, whilst ice-cooling, and the mixturewas stirred at room temperature for 1 hour and then left to stand for 2days. The solvent was then removed from the reaction mixture byevaporation under reduced pressure, and water was added to the residuethus obtained, after which it was extracted with ethyl acetate. Theextraction solution was washed with a saturated aqueous solution ofsodium chloride and dried over anhydrous sodium sulfate. The solvent wasthen removed from the extraction solution by evaporation under reducedpressure. The residue thus obtained was purified by silica gel columnchromatography, using 1:1 and 3:1 by volume mixtures of ethyl acetateand hexane as eluent. It was then recrystallized form a 1:2 by volumemixture of ethyl acetate and hexane, to obtain 154 mg of the titlecompound, melting at 91° C. to 92° C.

EXAMPLE 40 (R)-N-[5-(1,2-Dithiolan-3-yl)pentanoyl]methanesulfonamide(Compound No. 1-496) ##STR54##

110 mg of (R)-α-lipoic acid were dissolved in 2 ml of anhydrousdimethylformamide, and 97 mg of N,N'-carbonyldiimidazole were added tothe solution, whilst ice-cooling. The mixture was then stirred at roomtemperature for 4 hours. At the end of this time, 57 mg ofmethanesulfonamide and 26 mg of sodium hydride (as a 55% w/w dispersionin mineral oil) were added to the reaction mixture, whilst ice-cooling,and the mixture was stirred at room temperature for 5 hours and thenleft to stand overnight. The solvent was then removed from the reactionmixture by evaporation under reduced pressure, and water was added tothe residue this obtained. The resulting mixture was neutralized by theaddition of 2 N aqueous hydrochloric acid, after which it was extractedwith ethyl acetate. The extraction solution was washed with a saturatedaqueous solution of sodium chloride and then dried over anhydrous sodiumsulfate. The solvent was removed from the extraction solution byevaporation under reduced pressure. The residue thus obtained waspurified by silica gel column chromatography, using 1:1 and 3:1 byvolume mixtures of ethyl acetate and hexane as eluent, after which itwas dissolved in dioxane and lyophilised, to obtain 68 mg of the titlecompound, melting at 71° C. to 73° C.

EXAMPLE 41 4-[5-(1,2-Dithiolan-3-yl)pentanoyl]thiomorpholine (CompoundNo. 1-1133) ##STR55##

500 mg of D,L-α-lipoic acid were dissolved in 10 ml of anhydrousdimethylformamide, and then 422 mg of N,N'-carbonyldiimidazole wereadded to the solution. The mixture was then stirred at room temperaturefor 1 hour and 30 minutes, after which it was left to stand overnight.At the end of this time, 0.25 ml of thiomorpholine was added to thereaction mixture, and the mixture was stirred at room temperature for 5hours and then left to stand overnight. The solvent was then removedfrom the reaction mixture by evaporation under reduced pressure, andwater was added to the residue thus obtained, after which it wasextracted with ethyl acetate. The extraction solution was washed with asaturated aqueous solution of sodium chloride and dried over anhydroussodium sulfate. The solvent was then removed from the extractionsolution by evaporation under reduced pressure. The residue thusobtained was purified by silica gel column chromatography, using 1:1 and2:1 by volume mixtures of ethyl acetate and hexane as eluent. It wasthen dissolved in dioxane and lyophilised, to obtain 385 mg of the titlecompound as a yellow amorphous substance, melting at 31° C. to 32° C.

EXAMPLE 42 N-[4-(1,2-Dithiolan-3-yl)butyl]1-piperazinylcarboxamide(Compound No. 1-1141) ##STR56##

500 mg of D,L-α-lipoic acid were dissolved in 10 ml of anhydroustoluene, and then 0.36 ml of triethylamine and 0.56 ml ofdiphenylphosphoryl azide were added to the solution, after which theresulting mixture was stirred on an oil bath at 80° C. for 2 hours. Asolution of 1.03 g of piperazine in 10 ml of anhydrous dimethylformamidewas then added to the reaction mixture, whilst ice-cooling, and themixture was stirred at room temperature for 3 hours and 30 minutes andthen let to stand overnight. At the end of this time, the solvent wasremoved from the reaction mixture by evaporation under reduced pressure,and water was added to the residue thus obtained, after which it wasneutralised by the addition of 2 N aqueous hydrochloric acid. Thecrystals which precipitated were collected by filtration and washed withwater and ethyl acetate, to obtain 107 mg of the title compound meltingat 175° C. to 177° C.

EXAMPLE 43 3-[5-(1,2-Dithiolan-3-yl)pentanoyl]thiazolidine (Compound No.1-1258) ##STR57##

422 mg of n,N'-carbonyldiimidazole were added to a solution of 500 mg ofD,L-α-lipoic acid in 10 ml of anhydrous dimethylformamide. The resultingmixture was stirred at room temperature for 1 hour and 30 minutes. 0.20ml of thiazolidine was then added dropwise to the reaction mixture, andthen the mixture was stirred at room temperature for 4 hours. Thereaction mixture was allowed to stand overnight at room temperature andthen the solvent was removed by distillation under reduced pressure.Water was added to the residue, after which it was extracted with ethylacetate. The extract was washed with a saturated aqueous solution ofsodium chloride and then dried over anhydrous sodium sulfate. Ethylacetate was removed from the extract by distillation under reducedpressure, The residue was subjected to silica gel column chromatography,using 1:1, 3:1 and 1:0 by volume mixtures of ethyl acetate and hexane aseluent, followed by reverse phase preparative silica gel columnchromatography, using a 2:3 by volume mixture of acetonitrile and wateras eluent. Acetonitrile was removed from the eluate thus obtained bydistillation under reduced pressure, and the residue was extracted withethyl acetate. The extract was washed with a saturated aqueous solutionof sodium chloride and then dried over anhydrous sodium sulfate. Ethylacetate was removed from the extract by distillation under reducedpressure, and the resulting residue was dissolved in dioxane. Theresulting solution was lyophilised, to give 317 mg of the title compoundas a pale yellow amorphous substance, melting at 40 to 41° C.

EXAMPLE 44 N-[4-(1,2 -Dithiolan-3-yl)butyl]-N'-(1piperidyl)urea(Compound No. 1-1145) ##STR58##

0.36 ml of triethylamine and 0.56 ml of diphenylphosphoryl azide wereadded to a solution of 500 mg of D,L-α-lipoic acid in 10 ml of anhydroustoluene. The resulting mixture was stirred on an oil bath at 80° C. for1 hour and 30 minutes. 0.28 ml of 1-aminopiperidine was then addeddropwise to the reaction mixture, whilst ice-cooling, and then themixture was stirred at room temperature for 5 hours. The reactionmixture was then allowed to stand overnight at room temperature. Thesolvent was removed from the reaction mixture by distillation underreduced pressure. Water was added to the residue, after which it wasextracted with ethyl acetate. The extract was washed with a saturatedaqueous solution of sodium chloride and dried over anhydrous sodiumsulfate. Ethyl acetate was removed from the extract by distillationunder reduced pressure, and the residue was subjected to silica gelcolumn chromatography, using 1:0 and 5:1 by volume mixtures of ethylacetate and ethanol as eluent. The solvent was removed from the eluateby distillation under reduced pressure. The pressure was dissolved indioxane, after which it was lyophilised, to give 593 mg of the titlecompound as a yellow amorphous substance, melting at 67 to 69° C.

EXAMPLE 45

N-(1-Piperidyl)-5-(1,2-dithiolan-3-yl)pentanamide (Compound No. 1-1135)##STR59##

The reaction was effected as described in Example 43, but using 500 mgof D,L-α-lipoic acid, 10 of anhydrous dimethylformamide, 422 mg ofN,N'-carbonyldiimidazole and 0.28 ml of 1-aminopiperidine. The solventwas removed from the reaction mixture by distillation under reducedpressure. Water was added to the residue, after which it was extractedwith ethyl acetate. The extract was washed with a saturated aqueoussolution of sodium chloride and then dried over anhydrous sodiumsulfate. Ethyl acetate was removed from the extract by distillationunder reduced pressure. The residue was subjected to silica gel columnchromatography, using 2:1 and 1:0 by volume mixtures of ethyl acetateand hexane as eluent, after which it was recrystallised from ethylacetate, to give 298 mg of the title compound as a yellow needle-likecrystals, melting at 108 to 109° C.

EXAMPLE 46 Methyl 3-[4-(1,2-dithiolan-3-yl)butyl]ureidoacetate (CompoundNo. 1-739) ##STR60##

0.73 ml of triethylamine and 0.56 ml of diphenylphosphoryl azide wereadded to a solution of 500 mg of D,L-α-lipoic acid in 10 ml of anhydroustoluene. The resulting mixture was stirred on an oil bath at 80° C. for1 hour and 30 minutes. The solvent was then removed from the reactionmixture by distillation under reduced pressure. 10 ml of anhydrousdimethylformamide were then added to the residue, after which 301 mg ofL-glycine methyl ester hydrochloride were added, whilst ice-cooling. Theresulting mixture was then stirred at room temperature for one hour. Atthe end of this time, the reaction mixture was allowed to standovernight at room temperature, after which the solvent was removed bydistillation under reduced pressure. Water was added to the residue,which was then extracted with ethyl acetate. The extract was washed witha saturated aqueous solution of sodium chloride and then dried overanhydrous sodium sulfate. Ethyl acetate was removed from the extract bydistillation under reduced pressure, and the residue was subjected tosilica gel column chromatography, using 2:1 and 1:0 by volume mixturesof ethyl acetate and hexane as eluent, followed by reverse phasepreparative silica gel column chromatography, using 3:17, 3:7 and 3:2 byvolume mixtures of acetontrile and water as eluent. Acetonitrile wasremoved from the eluate so obtained by distillation under reducedpressure, and the residue was extracted with ethyl acetate. The extractwas washed with a saturated aqueous solution of sodium chloride and thendried over anhydrous sodium sulfate. Ethyl acetate was removed from theextract by distillation under reduced pressure. The residue wasdissolved in dioxane, after which it was lyophilised, to give 336 mg ofthe title compound as a pale yellow amorphous substance, melting at 62to 64° C.

EXAMPLE 47 Methyl [5-(1,2-dithiolan-3-yl)pentanoylamino]acetate(Compound No. 1-47) ##STR61##

422 mg of N,N'-carbonyldimidazole were added to a solution of 500 mg ofD,L-α-lipoic acid in 10 ml of anhydrous dimethylformamide. The resultingmixture was stirred at room temperature for 2 hours, after which 0.36 mlof triethylamine was added dropwise to the reaction mixture. 301 mg ofglycine methyl ester hydrochloride were then added to the reactionmixture, and then the mixture was stirred at room temperature for 1hour. The reaction mixture was allowed to stand at room temperature fortwo days, and then the solvent was removed by distillation under reducedpressure. Water was added to the residue, after which it was extractedwith ethyl acetate. The extract was washed with a saturated aqueoussolution of sodium chloride and then dried over anhydrous sodiumsulfate. Ethyl acetate was removed from the extract by distillationunder reduced pressure. The residue was subjected to silica gel columnchromatography, using 3:1 and 1:0 by volume mixtures of ethyl acetateand hexane as eluent, followed by reverse phase preparative silica gelcolumn chromatography, using 1:4, 3:7 and 1:1 by volume mixtures ofacetonitrile and water as eluent. Acetonitrile was removed from theeluate thus obtained by distillation under reduced pressure, and theresidue was extracted with ethyl acetate. The extract was washed with asaturated aqueous solution of sodium chloride and then dried overanhydrous sodium sulfate. Ethyl acetate was removed from the extract bydistillation under reduced pressure and the residue was dissolved indioxane, after which it was lyophilised, to give 320 mg of the titlecompound as a yellow oil having an Rf value of 0.26 (silica gel thinlayer chromatography; using a 3:1 by volume mixture of ethyl acetate andhexane as the developing solvent).

EXAMPLE 48 {3-[4-(1,2-Dithiolan-3-yl)butyl]ureido}acetic acid (CompoundNo. 1-738) ##STR62##

2.1 ml of a 1N aqueous solution of sodium hydroxide were added dropwiseto a solution of 218 mg of methyl{3-[4-(1,2-dithiolan-3-yl)butyl]ureido}acetate (prepared as described inExample 46) in 4 ml of methanol, and then the mixture was stirred atroom temperature for 5 hours. The reaction mixture was then allowed tostand overnight at room temperature, after which the solvent was removedfrom the reaction mixture by distillation under reduced pressure. Waterwas added to the residue. The resulting mixture was neutralized by theaddition of 2N aqueous hydrochloric acid, after which it was extractedwith ethyl acetate. The extract was washed with a saturated aqueoussolution of sodium chloride and then dried over anhydrous sodiumsulfate. Ethyl acetate was removed from the extract to distillationunder reduced pressure. The residue was recrystallized from a 3:1 byvolume mixture of ethyl acetate and hexane, to give 64 mg of the titlecompound as a pale yellow powder, melting at 95 to 96° C.

EXAMPLE 49 [4-(1,2-Dithiolan-3-yl)pentanoylamino]acetic acid (CompoundNo. 1-46) ##STR63##

0.28 g of methyl 5-(1,2-dithiolan-3-yl)pentanoylaminoacetate (preparedas described in Example 47) was dissolved in a mixture of 2 ml ofmethanol and 2 ml of tetrahydrofuran. 2.0 ml of a 1N aqueous solution ofsodium hydroxide were added dropwise to the resulting solution, and thenthe mixture was stirred at room temperature for 2 hours. The reactionmixture was then allowed to stand overnight at room temperature, afterwhich the solvent was removed from the reaction mixture by distillationunder reduced pressure. Water was added to the residue. The resultingmixture was neutralized by the addition of 2N aqueous hydrochloric acid,after which it was extracted with ethyl acetate. The extract was washedwith a saturated aqueous solution of sodium chloride and then dried overanhydrous sodium sulfate. Ethyl acetate was removed from the extract bydistillation under reduced pressure. The residue was dissolved indioxane, after which it was lyophilised, to give 156 mg of the titlecompound as a yellow oil having an Rf value of 0.12 (silica gel thinlayer chromatography; using a 5:1 by volume mixture of ethyl acetate andmethanol as the developing solvent).

EXAMPLE 50 Methyl 2(S)-{3-[4-(1,2-dithiolan-3-yl)butyl]ureido}propionateCompound No. 1-742) ##STR64##

The reaction was effected as described in Example 46, but using 500 mgof D,L-α-lipoic acid, 10 ml of anhydrous toluene, 0.73 ml oftriethylamine, 0.56 ml of diphenylphosphoryl azide, 10 ml of anhydrousdimethylformamide and 335 mg of L-alanine methyl ester hydrochloride.The solvent was removed from the reaction mixture by distillation underreduced pressure. Water was added to the residue, after which it wasextracted with ethyl acetate. The extract was washed with a saturatedaqueous solution of sodium chloride and then dried over anhydrous sodiumsulfate. Ethyl acetate was removed from the extract by distillationunder reduced pressure and the residue was subjected to silica gelcolumn chromatography, using 2:1 and 1:0 by volume mixtures of ethylacetate and hexane as eluent. Ethyl acetate was removed from the eluateby distillation under reduced pressure, and the residue wasrecrystallized from a 1:1:1 by volume mixture of ethyl acetate,diisopropyl ether and hexane, to give 142 mg of the title compound asyellow crystals, melting at 90 to 92° C.

EXAMPLE 51 Methyl 2(S)-[5-(1,2-dithiolan-3-yl)pentanoylamino]propionateCompound No. 1-50) ##STR65##

The reaction was effected as described in Example 47, but using 500 mgof D,L-α-lipoic acid, 10 ml of anhydrous dimethylformamide, 422 mg ofN,N'-carbonyldiimidazole, 0.36 ml of triethylamine and 335 mg ofL-alanine methyl ester hydrochloride. The solvent was removed from thereaction mixture by distillation under reduced pressure. Water was addedto the residue, after which it was extracted with ethyl acetate. Theextract was washed with a saturated aqueous solution of sodium chlorideand then dried over anhydrous sodium sulfate. Ethyl acetate was removedfrom the extract by distillation under reduced pressure. The residue wassubjected to silica gel column chromatography, using a 2:1 by volumemixture of ethyl acetate and hexane as eluent, followed by reverse phasepreparative silica gel column chromatography, using by volume 3:7 and1:1 mixtures of acetonitrile and water as eluent. Acetonitrile wasremoved from the eluate so obtained by distillation under reducedpressure, and the residue was extracted with ethyl acetate. The extractwas washed with a saturated aqueous solution of sodium chloride and thendried over anhydrous sodium sulfate. Ethyl acetate was removed from theextract by distillation under reduced pressure. The residue wasdissolved in dioxane, after which it was lyophilised, to give 271 mg ofthe title compound as a pale yellow amorphous substance, melting at 48to 49° C.

EXAMPLE 52 2(S)-{3-[4-(1,2-Dithiolan-3yl)butyl]ureido}propionic acidCompound No. 1-740) ##STR66##

The reaction was effected as described in Example 46, but using 1.00 gof D,L-α-lipoic acid, 20 ml of anhydrous toluene, 1.47 ml oftriethylamine, 1.14 ml of diphenylphosphoryl azide, 740 mg of L-alaninemethyl ester hydrochloride and 20 ml of anhydrous dimethylformamide. Thesolvent was removed from the reaction mixture by distillation underreduced pressure. Water was added to the residue, after which it wasextracted with ethyl acetate. The extract was washed with a saturatedaqueous solution of sodium chloride and dried over anhydrous sodiumsulfate. Ethyl acetate was removed from the extract by distillationunder reduced pressure. The residue was subjected to silica gel columnchromatography, using 2:1 and 1:0 by volume mixtures of ethyl acetateand hexane as eluent, after which it was recrystallised from ethylacetate, to give 0.80 g of yellow crystals.

The resulting crystals were dissolved in a mixture of 10 of methanol and3 ml of tetrahydrofuran, and then 16.8 ml of a 1N aqueous solution ofsodium hydroxide were added dropwise thereto. The resulting mixture wasstirred at room temperature for 6 hours and 30 minutes. The solvent wasthen removed from the reaction mixture by distillation under reducedpressure. Water was added to the residue. The resulting mixture wasneutralized by the addition of 2N aqueous hydrochloric acid, after whichit was extracted with ethyl acetate. The extract was washed with asaturated aqueous solution of sodium chloride and then dried overanhydrous sodium sulfate. Ethyl acetate was removed from the extract bydistillation under reduced pressure and the residue was recrystallizedfrom ethyl acetate, to give 141 mg of the title compound as pale yellowcrystals, melting at 128 to 130° C.

EXAMPLE 53 2(S)-[1,2-dithiolan-3-yl)pentanoylamino]propionic acid(Compound No. 1-48) ##STR67##

The reaction was effected as described in Example 49, but using (153 mgof methyl 2(S)-[5-(1,2-dithiolan-3-yl)pentanoylamino]propionate(prepared as described in Example 51), 3 ml of methanol and 1.3 ml of a1N aqueous solution of sodium hydroxide. The solvent was removed fromthe reaction mixture by distillation under reduced pressure. Water wasadded to the residue. The resulting mixture was neutralized by theaddition of 2N aqueous hydrochloric acid, after which it was extractedwith ethyl acetate. The extract was washed with a saturated aqueoussolution of sodium chloride and then dried over anhydrous sodiumsulfate. Ethyl acetate was removed from the extract by distillationunder reduced pressure. The residue was dissolved in dioxane, afterwhich it was lyophilised, to give 90 mg of the title compound as ayellow oil having an Rf value of 0.18 (silica gel thin layerchromatography; using ethyl acetate as the developing solvent).

EXAMPLE 54 Methyl 3-{3-[4-(1,2-dithiolan-3-yl)butyl]ureido}propionate(Compound No. 1-741 methyl ester) ##STR68##

The reaction was effected as described in Example 46, but using 500 mgof D,L-α-lipoic acid, 10 ml of anhydrous toluene, 0.74 ml oftriethylamine, 0.56 ml of diphenylphosphoryl azide, 335 mg of α-alaninemethyl ester hydrochloride and 10 ml of anhydrous dimethylformamide. Thesolvent was removed from the reaction mixture by distillation underreduced pressure. Water was added to the residue, after which it wasextracted with ethyl acetate. The extract was washed with a saturatedaqueous solution of sodium chloride and then dried over anhydrous sodiumsulfate. Ethyl acetate was removed from the extract by distillationunder reduced pressure and the residue was subjected to silica gelcolumn chromatography, using 3:1 and 1:0 by volume mixtures of ethylacetate and hexane as eluent, after which it was recrystallised from a1:2 by volume mixture of ethyl acetate and hexane, to give 213 mg of thetitle compound as yellow crystals, melting at 67 to 69° C.

EXAMPLE 55 Methyl 3-[5-(1,2-dithiolan-3-yl)pentanoylamino]propionate(Compound No. 1-49 methyl ester) ##STR69##

The reaction was effected as described in Example 47, but using 500 mgof D,L-α-lipoic acid, 10 ml of anhydrous dimethylformamide, 422 mg ofN,N'-carbonyldiimidazole, 0.36 ml of triethylamine and 335 mg ofβ-alanine methyl ester hydrochloride. The solvent was removed from thereaction mixture by distillation under reduced pressure. Water was addedto the residue, after which it was extracted with ethyl acetate. Theextract was washed with a saturated aqueous solution of sodium chlorideand then dried over anhydrous sodium sulfate. Ethyl acetate was removedfrom the extract by distillation under reduced pressure. The residue wassubjected to silica gel column chromatography, using 2:1 and 1:0 byvolume mixtures of ethyl acetate and hexane as eluent, after which itwas recrystallized from a 1:2 by volume mixture of ethyl acetate andhexane, to give 333 mg of the title compound as a yellow plate-likecrystals, melting at 54 to 55° C.

EXAMPLE 56 3-{3-(4-(1,2-Dithiolan-3-yl)butyl]ureido}propionic acid(Compound No. 1-741) ##STR70##

The reaction was effected as described in Example 48, but using 115 mgof methyl 3-{3-[4-(1,2-dithiolan-3-yl)butyl]ureido}propionate (preparedas described in Example 54), 3 ml of methanol, 2 ml of tetrahydrofuranand 1.40 ml of a 1N aqueous solution of sodium hydroxide. The solventwas removed from the reaction mixture by distillation under reducedpressure. Water was added to the residue. The resulting mixture wasneutralized by the addition of 2N aqueous hydrochloric acid, after whichit was extracted with ethyl acetate. The extract was washed with asaturated aqueous solution of sodium chloride and then dried overanhydrous sodium sulfate. Ethyl acetate was removed from the extract bydistillation under reduced pressure and the crystals so precipitatedwere collected by filtration, to give 70 mg of the title compound as ayellow powder, melting at 108 to 110° C.

EXAMPLE 57 3-[5-(1,2-Dithiolan-3-yl)pentanoylamino]propionic acid(Compound No. 1-49) ##STR71##

The reaction was effected as described in Example 49, but using 213 mgof methyl 3-[5-(1,2-dithiolan-3-yl)pentanoylamino]propionate (preparedas described in Example 55), 4 ml of methanol and 1.80 ml of a 1Naqueous solution of sodium hydroxide. The solvent was removed from thereaction mixture by distillation under reduced pressure. Water was addedto the residue. The resulting mixture was neutralized by the addition of2N aqueous hydrochloric acid, after which it was extracted with ethylacetate. The extract was washed with a saturated aqueous solution ofsodium chloride and then dried over anhydrous sodium sulfate. Ethylacetate was removed from the extract by distillation under reducedpressure. The residue was dissolved in dioxane, after which it waslyophilised, to give 0.11 g of the title compound as a pale yellowamorphous substance, melting at 74 to 76° C.

EXAMPLE 58 2-[5-(1,2-Dithiolan-3-yl)pentyl]isoindole-1,3-dione (CompoundNo. 1-2606) ##STR72##

3.25 ml of dimethyl azodicarboxylate were added dropwise to a solutionof 5.77 g of triphenylphosphine in 20 ml of tetrahydrofuran, whilstice-cooling, and then the mixture was stirred at room temperature for 30minutes. 3.24 g of phthalimide were then added to the reaction mixture,after which a mixture of 20 mmol of 5-(1,2-dithiolan-3-yl)pentanol(prepared as described in Preparation 1) in 30 ml of toluene and 10 mlof tetrahydrofuran was added dropwise, and the mixture was stirred atroom temperature for one hour. The reaction mixture was allowed to standovernight at room temperature, after which 1.57 g of triphenylphosphineand 0.89 ml of dimethyl azodicarboxylate were added. The resultingmixture was stirred at room temperature for 7 hours and 30 minutes. 0.88g of phthalimide, 1.57 g of triphenylphosphine and 0.89 ml of dimethylazodicarboxylate were then added to the reaction mixture. The reactionmixture was allowed to stand at room temperature for 4 days. At the endof this time, the solvent was removed from the reaction mixture bydistillation under reduced pressure, and the residue was subjected tosilica gel column chromatography, using 1:6 and 1:4 by volume mixturesof ethyl acetate and hexane as eluent. The solvent was removed from theeluate by distillation under reduced pressure, and 30 ml of toluene wereadded to the residue. 1 ml of the resulting mixture was weighed, and thesolvent was removed from it by distillation under reduced pressure, togive 165 mg of the title compound as an orange oil having an Rf value of0.35 (silica gel thin layer chromatography; using a 1:4 by volumemixture of ethyl acetate and hexane as the developing solvent).

EXAMPLE 59 N-[5-(1,2-Dithiolan-3-yl)pentyl]methanesulfonamide (CompoundNo. 1-2470) ##STR73##

1 ml of butylamine was added to a solution of 0.24 g of2-[5-(1,2-dithiolan-3-yl)pentyl]isoindole-1,3-dione in 1 ml of methanol.The resulting mixture was stirred at room temperature for 6 hours. Thereaction mixture was then allowed to stand overnight at roomtemperature. At the end of this time, the solvent was removed from thereaction mixture by distillation under reduced pressure. Water was addedto the residue, after which it was extracted with ethyl acetate. Theextract was washed with a saturated aqueous solution of sodium chlorideand then dried over anhydrous sodium sulfate. Ethyl acetate was removedfrom the extract by distillation under reduced pressure. 2 ml oftetrahydrofuran were added to the residue, and then 0.22 ml oftriethylamine and 0.12 ml of methanesulfonyl chloride were addeddropwise thereto, whist ice-cooling. The mixture was then stirred atroom temperature for 3 hours. At the end of this time, the solvent wasremoved from the reaction mixture by distillation under reducedpressure. Water was added to the residue, after which it was extractedwith ethyl acetate. The extract was washed with a saturated aqueoussolution of sodium chloride and then dried over anhydrous sodiumsulfate. Ethyl acetate was removed from the extract by distillationunder reduced pressure, and the residue was subjected to silica gelcolumn chromatography, using 1:1 and 2:1 by volume mixtures of ethylacetate and hexane as eluent, followed by reverse phase preparativesilica gel column chromatography, using a 1:1 by volume mixture ofacetontrile and water as eluent. Acetonitrile was removed from theeluate so obtained by distillation under reduced pressure, and theresidue was extracted with ethyl acetate. The extract was washed with asaturated aqueous solution of sodium chloride and then dried overanhydrous sodium sulfate. Ethyl acetate was removed from the extract bydistillation under reduced pressure, and the residue was dissolved indioxane, after which it was lyophilised, to give 100 mg of the titlecompound as a pale yellow amorphous substance, melting at 43 to 46° C.

EXAMPLE 60 N-[5-(1,2-Dithiolan-3-yl)pentyl]acetamide (Compound No.1-1962) ##STR74##

1 ml of butylamine was added to a mixture of 1.3 mmol of2-[5-(1,2-dithiolan-3-yl)pentyl]isoindole-1,3-dione, 9 ml of toluene and2 ml of methanol. The resulting mixture was stirred at room temperaturefor 3 hours, after which the reaction mixture was allowed to stand atroom temperature for 2 days. 1 ml of butylamine was then added to thereaction mixture. The resulting mixture was stirred at room temperaturefor 3 hours. The solvent was then removed from the reaction mixture bydistillation under reduced pressure. Water was added to the residue,after which it was extracted with ethyl acetate. The extract was washedwith a saturated aqueous solution of sodium chloride and then dried overanhydrous sodium sulfate. Ethyl acetate was removed from the extract bydistillation under reduced pressure. 5 ml of anhydrous tetrahydrofuranwere then added to the residue. 0.28 ml of triethylamine and 0.14 ml ofacetyl chloride were then added to dropwise to the resulting mixture,whilst ice-cooling, and then the mixture was stirred at room temperaturefor 1 hour and 30 minutes. At the end of this time, the solvent wasremoved from the reaction mixture by distillation under reducedpressure. Water was added to the residue, after which it was extractedwith ethyl acetate. The extract was washed with a saturated aqueoussolution of sodium chloride and then dried over anhydrous sodiumsulfate. Ethyl acetate was removed from the extract by distillationunder reduced pressure. The residue was subjected to silica gel columnchromotagraphy, using 1:0 and 10:1 by volume mixtures of ethyl acetateand methanol as eluent. The solvent was removed from the eluate bydistillation under reduced pressure. The residue was dissolved indioxane, after which it was lyophilised, to give 161 mg of the titlecompound as yellow crystals, melting at 28 to 33° C.

EXAMPLE 61 N-[5-(1,2-Dithiolan-3-yl)pentyl]propionamide (Compound No.1-1963) ##STR75##

2 ml of methanol and 2 ml of butylamine were added to a solution of 1.6mmol of 2-[5(1,2-dithiolan-3-yl)pentyl]isoindole-1,3-dione in 3 ml oftoluene. The resulting mixture was stirred at room temperature for 6hours. The reaction mixture was then allowed to stand overnight at roomtemperature. At the end of this time, the solvent was removed from thereaction mixture by distillation under reduced pressure. Water was addedto the residue, after which it was extracted with ethyl acetate. Theextract was washed with a saturated aqueous solution of sodium chlorideand then dried over anhydrous sodium sulfate. Ethyl acetate was removedfrom the extract by distillation under reduced pressure. 5 ml ofpyridine were then added to the residue. 0.31 ml of propionic anhydridewas added dropwise to the resulting mixture, and then the mixture wasstirred at room temperature for 2 hours and 30 minutes. The solvent wasremoved from the reaction mixture by distillation under reducedpressure. Water was added to the residue after which it was extractedwith ethyl acetate. The extract was washed with a saturated aqueoussolution of sodium chloride and then dried over anhydrous sodiumsulfate. Ethyl acetate was removed from the extract by distillationunder reduced pressure. The residue was thereafter subjected to silicagel column chromatography, using 2:1, 3:1 and 1:0 by volume mixtures ofethyl acetate and hexane as eluent, followed by reverse phasepreparative silica gel column chromatography, using 1:4, 3:7, 2:3 and1:1 by volume mixtures of acetonitrile and water as eluent. Acetonitrilewas removed from the eluate so obtained by distillation under reducedpressure, and the residue was extracted with ethyl acetate. The extractwas washed with a saturated aqueous solution of sodium chloride and thendried over anhydrous sodium sulfate. Ethyl acetate was removed from theextract by distillation under reduced pressure. The residue wasdissolved in dioxane, after which it was lyophilised, to give 125 mg ofthe title compound as a yellow oil having an Rf value of 0.45 (silicagel thin layer chromatography; using ethyl acetate as the developingsolvent).

EXAMPLE 62 [5-(1,2-Dithiolan-3-yl)pentyl]urea (Compound No. 1-1993)##STR76##

2 ml of methanol and 2 ml of butylamine were added to a solution of 1:6mmol of 2-[5-(1,2-dithiolan-3-yl)pentyl]isoindole-1,3-dione in 3 ml oftoluene. The resulting mixture was stirred at room temperature for 5hours and 30 minutes. The reaction mixture was then allowed to standovernight at room temperature. At the end of this time, the solvent wasremoved from the reaction mixture by distillation under reducedpressure. Water was added to the resulting residue, after which it wasextracted with ethyl acetate. The extract was washed with a saturatedaqueous solution of sodium chloride and then dried over anhydrous sodiumsulfate. Ethyl acetate was removed from the extract by distillationunder reduced pressure. 5 ml of tetrahydrofuran were added to theresidue. 0.32 ml of trimethylsilyl isocyanate was then added dropwise tothe resulting mixture, whilst ice-cooling, and then the mixture wasstirred at room temperature for 3 hours and 30 minutes. At the end ofthis time, the solvent was removed from the reaction mixture bydistillation under reduced pressure. Water was added to the residue,after which it was extracted with ethyl acetate. The extract was washedwith a saturated aqueous solution of sodium chloride and then dried overanhydrous sodium sulfate. Ethyl acetate was removed from the extract bydistillation under reduced pressure and the residue was subjected tosilica gel column chromatography, using 1:0 and 5:1 by volume mixturesof ethyl acetate and methanol as eluent. The solvent was removed fromthe eluate by distillation under reduced pressure. The residue wasrecrystallized from ethyl acetate, to give 80 mg of the title compoundas yellow crystals, melting at 74 to 78° C.

EXAMPLE 63 1-[5-(1,2-Dithiolan-3-yl)pentyl]-3-methylthiourea (CompoundNo. 1-2567) ##STR77##

The reaction was effected as described in Example 62, but using asolution of 1.5 mmol of2-[5-(1,2-dithiolan-3yl)pentyl]isoindole-1,3-dione in 3 ml of toluene, 2ml of methanol, 2 ml of butylamine, 5 ml of anhydrous tetrahydrofuranand 0.12 ml of methyl isothiocyanate. The solvent was removed from thereaction mixture by distillation under reduced pressure. Water was addedto the residue, after which it was extracted with ethyl acetate. Theextract was washed with a saturated aqueous solution of sodium chlorideand then dried over anhydrous sodium sulfate. Ethyl acetate was removedfrom the extract by distillation under reduced pressure. The residue wassubjected to silica gel column chromatography, using 1:0 and 20:1 byvolume mixtures of ethyl acetate and methanol as eluent, followed byreverse phase preparative silica gel column chromatography, using 3:7and 1:1 by volume mixtures of acetonitrile and water as eluent.Acetonitrile was removed from the eluate so obtained by distillationunder reduced pressure. The residue was thereafter extracted with ethylacetate. The extract was washed with a saturated aqueous solution ofsodium chloride and then dried over anhydrous sodium sulfate. Ethylacetate was removed from the extract by distillation under reducedpressure. The residue was recrystallized from a 1:1 by volume mixture ofethyl acetate and hexane, to give 183 mg of the title composed as yellowcrystals, melting at 64 to 65° C.

EXAMPLE 64 Ethyl [5-(1,2-dithiolan-3-yl)pentyl]carbamate (Compound No.1-1977) ##STR78##

2 ml of methanol and 2 ml of butylamine were added to a solution of 1.6mmol of 2-[5-(1,2-dithiolan-3-yl)pentyl]isoindole-1,3-dione in 3 ml oftoluene. The resulting mixture was stirred at room temperature for 7hours. At the end of this time, the reaction mixture was allowed tostand overnight at room temperature. The solvent was then removed fromthe reaction mixture by distillation under reduced pressure. Water wasadded to the resulting residue, after which it was extracted with ethylacetate. The extract was washed with a saturated aqueous solution ofsodium chloride and then dried over anhydrous sodium sulfate. Ethylacetate was removed from the extract by distillation under reducedpressure. 2 ml of anhydrous tetrahydrofuran were added to the residue,and then 0.33 ml of triethylamine and 0.23 ml of ethyl chloroformatewere added dropwise, whilst ice-cooling. The resulting mixture wasstirred at room temperature for 2 hours. The solvent was then removedfrom the reaction mixture by distillation under reduced pressure. Waterwas added to the residue, after which it was extracted with ethylacetate. The extract was washed with a saturated aqueous solution ofsodium chloride and then dried over anhydrous sodium sulfate. Ethylacetate was removed from the extract by distillation under reducedpressure, and the residue was subjected to silica gel columnchromatography, using 1:3 and 1:2 by volume mixtures of ethyl acetateand hexane as eluent, followed by reverse phase preparative silica gelcolumn chromatography, using a 1:1 by volume mixture of acetonitrile andwater as eluent. Acetonitrile was removed from the eluate so obtained bydistillation under reduced pressure, and the residue was extracted withethyl acetate. The extract was washed with a saturated aqueous solutionof sodium chloride and then dried over anhydrous sodium sulfate. Ethylacetate was removed from the extract by distillation under reducedpressure. The residue was dissolved in dioxane, after which it waslyophilised, to give 75 mg of the title compound as a red oil having anRf value of 0.46 (silica gel thin layer chromatography; using a 1:2 byvolume mixture of ethyl acetate and hexane as the developing solvent).

EXAMPLE 65 Methyl N-[5-(1,2-dithiolan-3-yl)pentyl]oxalamidate (CompoundNo. 1-2590) ##STR79##

2 ml of methanol and 2 ml of butylamine were added to a solution of 1.5mmol of 2-[5-(1,2-dithiolan-3-yl)pentyl]isoindole1,3-dione in 3 ml oftoluene. The resulting mixture was stirred at room temperature for onehour. The reaction mixture was then allowed to stand overnight at roomtemperature. At the end of this time, the solvent was removed from thereaction mixture by distillation under reduced pressure. Water was addedto the residue, after which it was extracted with ethyl acetate. Theextract was washed with a saturated aqueous solution of sodium chlorideand then dried over anhydrous sodium sulfate. Ethyl acetate was removedfrom the extract by distillation under reduced pressure. 4 ml ofanhydrous tetrahydrofuran were added to the residue, and then 0.32 ml oftriethylamine and 0.21 ml of methyloxalyl acid chloride were addeddropwise, whist ice-cooling. The resulting mixture was stirred at roomtemperature for 2 hours. At the end of this time, the solvent wasremoved from the reaction mixture by distillation under reducedpressure. Water was added to the residue, after which it was extractedwith ethyl acetate. The extract was washed with a saturated aqueoussolution of sodium chloride and then dried over anhydrous sodiumsulfate. Ethyl acetate was removed from the extract by distillationunder reduced pressure and the residue was subjected to reverse phasepreparative silica gel column chromatography, using a 2:3 by volumemixture of acetonitrile and water as eluent. Acetonitrile was removedfrom the eluate so obtained by distillation under reduced pressure. Theresidue was thereafter extracted with ethyl acetate. The extract waswashed with a saturated aqueous solution of sodium chloride and thendried over anhydrous sodium sulfate. Ethyl acetate was removed from theextract by distillation under reduced pressure. The residue wasdissolved in dioxane, after which it was lyophilised, to give 154 mg ofthe title compound as a pale yellow amorphous substance, melting at 42to 43° C.

EXAMPLE 66 N-[5-(1,2-Dithiolan-3-yl)pentyl]succinamic acid (Compound No.1-1970) ##STR80##

The reaction was effected as described in Example 61, but using asolution of 1.5 mmol of2-[5-(1,2-dithiolan-3-yl)pentyl]isoindole-1,3-dione in 3 ml of toluene,2 ml of methanol, 2 ml of butylamine, 4 ml of pyridine and 230 mg ofsuccinic anhydride. The solvent was removed from the reaction mixture bydistillation under reduced pressure. Water was added to the residue,after which it was extracted with ethyl acetate. The extract was washedwith a saturated aqueous solution of sodium chloride and then dried overanhydrous sodium sulfate. Ethyl acetate was removed from the extract bydistillation under reduced pressure and the residue was subjected toreverse phase preparative silica gel column chromatography, using 2:3,1:1 and 3:2 by volume mixtures of acetonitrile and water as eluent.Acetonitrile was removed from the eluate so obtained by distillationunder reduced pressure. The residue was extracted with ethyl acetate.The extract was washed with a saturated aqueous solution of sodiumchloride and then dried over anhydrous sodium sulfate. Ethyl acetate wasremoved from the extract by distillation under reduced pressure. Theresidue was dissolved in dioxane, after which it was lyophilised, togive 166 mg of the title compound as a pale yellow amorphous substance,melting at 74° C.

EXAMPLE 67 4-[5-(1,2-Dithiolan-3-yl)pentylcarbamoyl]butanoic acid(Compound No. 1-2577) ##STR81##

The reaction was effected as described in Example 61, but using asolution of 1.5 mmol of2-[5-(1,2-dithiolan-3-yl)pentyl]isoindole-1,3-dione in 3 ml of toluene,2 ml of methanol, 2 ml of butylamine, 4 ml of pyridine and 262 mg ofglutaryl anhydride. The solvent was removed from the reaction mixture bydistillation under reduced pressure. Water was added to the residue,after which it was extracted with ethyl acetate. The extract was washedwith a saturated aqueous solution of sodium chloride and then dried overanhydrous sodium sulfate. Ethyl acetate was removed from the extract bydistillation under reduced pressure and the residue was subjected toreverse phase preparative silica gel column chromatography, using a 2:3by volume mixture of acetonitrile and water as eluent. Acetonitrile wasremoved from the eluate so obtained by distillation under reducedpressure. The residue was then extracted with ethyl acetate. The extractwas washed with a saturated aqueous solution of sodium chloride and thendried over anhydrous sodium sulfate. Ethyl acetate was removed from theextract by distillation under reduced pressure. The residue wasdissolved in dioxane, after which it was lyophilised, to give 132 mg ofthe title compound as a pale yellow amorphous substance, melting at 60to 62° C.

EXAMPLE 68 Methyl [5-(1,2-dithiolan-3-yl)pentylamino]acetate (CompoundNo. 1-2584) ##STR82##

2 ml of methanol and 2 ml of butylamine were added to a solution of 1.6mmol of 2-[5-(1,2-dithiolan-3-yl)pentyl]isoindole-1,3-dione in 3 ml oftoluene. The resulting mixture was allowed to stand overnight at roomtemperature. The solvent was then removed from the reaction mixture bydistillation under reduced pressure. Water was added to the resultingresidue, after which it was extracted with ethyl acetate. The extractwas washed with a saturated aqueous solution of sodium chloride and thendried over anhydrous sodium sulfate. Ethyl acetate was removed from theextract by distillation under reduced pressure. 4 ml of anhydroustetrahydrofuran were added to the residue, and then 0.33 ml oftriethylamine and 0.17 ml of methyl bromoacetate were added dropwise,whilst ice-cooling. The resulting mixture was stirred for one hour,whilst ice-cooling and then for 5 hours at room temperature. Thereaction mixture was then allowes to stand at room temperature for 2days. At the end of this time, the solvent was removed from the reactionmixture by distillation under reduced pressure. Water was added to theresidue, after which it was extracted with ethyl acetate. The extractwas washed with a saturated aqueous solution of sodium chloride and thendried over anhydrous sodium sulfate. Ethyl acetate was removed from theextract by distillation under reduced pressure, and the residue wassubjected to silica gel column chromatography, using 1:0 and 20:1 byvolume mixtures of ethyl acetate and methanol as eluent. The solvent wasremoved from the eluate so obtained by distillation under reducedpressure. The residue was dissolved in dioxane, after which it waslyophilised, to give 195 mg of the title compound as a yellow oil havingan Rf value of 0.55 (silica gel thin layer chromatography; using a 4:1by volume mixture of ethyl acetate and methanol as the developingsolvent.

EXAMPLE 69 Methyl 3-[5-(1,2-dithiolan-3-yl)pentylamino]propionate(Compound No. 1-2586 methyl ester) ##STR83##

The reaction was effected as described in Example 68, but using asolution of 1.5 mmol of2-[5-(1,2-dithiolan-3-yl)pentyl]isoindole-1,3-dione, 2 ml of methanol, 2ml of butylamine, 4 ml of anhydrous tetrahydrofuran, 0.24 ml oftriethylamine and 0.19 ml of methyl bromopropionate. The solvent wasremoved from the reaction mixture by distillation under reducedpressure. Water was added to the residue, after which it was extractedwith ethyl acetate. The extract was washed with a saturated aqueoussolution of sodium chloride and then dried over anhydrous sodiumsulfate. Ethyl acetate was removed from the extract by distillationunder reduced pressure. The residue was subjected to silica gel columnchromatography, using 1:0, 20:1 and 4:1 by volume mixtures of ethylacetate and methanol as eluent. The solvent was removed from the eluateso obtained by distillation under reduced pressure. The residue wasdissolved in dioxane, after which it was lyophilised, to give 161 mg ofthe title compound as a yellow oil having an Rf value of 0.21 (silicagel thin layer chromatography, using a 4:1 by volume mixture of ethylacetate and methanol as the developing solvent).

EXAMPLE 70 Methyl 2(R)-{3-[4-(1,2-dithiolan-3-yl)butyl]ureido}propionate(Compound No. 1-742) ##STR84##

The reaction was effected as described in Example 46, but using 0.51 gof D,L-α-lipoic acid, 10 ml of anhydrous toluene, 0.75 ml oftriethylamine, 0.59 ml of diphenylphosphoryl azide, 10 ml of anhydrousdimethylformamide and 0.34 g of D-alanine methyl ester hydrochloride.The solvent was removed from the reaction mixture by distillation underreduced pressure. Water was added to the residue, after which it wasextracted with ethyl acetate. The extract was washed with a saturatedaqueous solution of sodium chloride and then dried over anhydrous sodiumsulfate. Ethyl acetate was removed from the extract by distillationunder reduced pressure. The residue was subjected to silica gel columnchromatography, using 1:1 and 1:0 by volume mixtures of ethyl acetateand hexane as eluent. The solvent was removed from the eluate soobtained by distillation under reduced pressure. The residue wasdissolved in dioxane, after which it was lyophilised, to give 0.27 g ofthe title compound as a yellow powder melting at 72 to 82° C.

EXAMPLE 71 2(R)-{3-[4-(1,2-Dithiolan-3-yl)butyl]ureido}propionic acid(Compound No. 1-740) ##STR85##

The reaction was effected as described in Example 48, but using 1.74 gof methyl 2(R)-{3-[4-(1,2-dithiolan-3-yl)butyl]ureido}propionate(prepared as described in Example 70), 30 ml of methanol, 22 ml oftetrahydrofuran and 17.0 ml of a 1N aqueous solution of sodiumhydroxide. The solvent was removed from the reaction mixture bydistillation under reduced pressure. Water was added to the residue.After neutralisation with 2N aqueous hydrochloric acid, the mixture wasextracted with ethyl acetate. The extract was washed with a saturatedaqueous solution of sodium chloride and then dried over anhydrous sodiumsulfate. Ethyl acetate was removed from the extract by distillationunder reduced pressure. The residue was recrystallized from ethylacetate, to give 0.56 g of the title compound as yellow crystals,melting at 131 to 134° C.

EXAMPLE 72N-(2-{3-[4-(1,2-Dithiolan-3-yl)butyl]ureido}propionyl)methanesulfonamide(Compound No. 1-1280) ##STR86## (a) 127 mg of N,N'-carbonyldimidazolewere added to a solution of 208 mg of2(R)-{3-[4-(1,2-dithiolan-3-yl)butyl]ureido}propionic acid (prepared asdescribed in Example 71) in 2 ml of anhydrous dimethylformamide, andthen the mixture was stirred at room temperature for 3 hours and 10minutes.

(b) Meanwhile, 34 mg of sodium hydride (as a 55% w/w dispersion inmineral oil) were washed with hexane, and then 3 ml of anhydrousdimethylformamide were added. 74 mg of methanesulfonamide were added tothe resulting mixture, whilst ice-cooling, and then the mixture wasstirred at room temperature for 3 hours and 45 minutes. At the end ofthis time, the solution prepared as described in step (a) above wasadded dropwise to the reaction mixture, and the resulting mixture wasstirred at room temperature for 4 hours. The reaction mixture was thenallowed to stand overnight at room temperature. The solvent was thenremoved from the reaction mixture by distillation under reducedpressure. Water was added to the residue. After neutralisation with 2 Naqueous hydrochloric acid, the resulting mixture was extracted withethyl acetate. The extract was washed with a saturated aqueous solutionof sodium chloride and then dried over anhydrous sodium sulfate. Ethylacetate was removed from the extract by distillation under reducedpressure. The residue was recrystallized from methanol, to give 77 mg ofthe title compound as a pale yellow powder, melting at 140 to 150° C.

EXAMPLE 73 Methyl 4-[5-(1,2-dithiolan-3-yl)pentanoylamino]butanoate(Compound No. 1-1275 methyl ester) ##STR87## (a) 0.86 g ofN,N'-carbonyldimidazole was added to a solution of 1.00 g ofD,L-α-lipoic acid in 20 ml of anhydrous dimethylformamide, whilstice-cooling. The resulting mixture was stirred at room temperature for 1hour and 25 minutes.

(b) Meanwhile, 0.23 g of sodium hydride (as a 55% w/w dispersion inmineral oil) was washed with hexane, after which 20 ml of anhydrousdimethylformamide were added. 0.82 of methyl 4-aminobutanoatehydrochloride was then added, whilst ice-cooling, and then the resultingmixture was stirred at room temperature for 1 hour and 45 minutes. Thesolution prepared as described in step (a) above was then added dropwiseto the reaction mixture, whilst ice-cooling, and then the mixture wasstirred at room temperature for 1 hour and 30 minutes. The reactionmixture was allowed to stand overnight at room temperature, after whichthe solvent was removed from the reaction mixture by distillation underreduced pressure. Water was added to the residue. After neutralisationwith 2N aqueous hydrochloric acid, the resulting mixture was extractedwith ethyl acetate. The extract was washed with a saturated aqueoussolution of sodium chloride and then dried over anhydrous sodiumsulfate. Ethyl acetate was removed from the extract by distillationunder reduced pressure, and the residue was subjected to silica gelcolumn chromatography, using 1:1 and 1:0 by volume mixtures of ethylacetate and hexane as eluent. The ethyl acetate was removed from theeluate so obtained by distillation under reduced pressure. The residuewas dissolved in dioxane, after which it was lyophilised, to give 0.83 gof the title compound as a yellow powder, melting at 30 to 32° C.

EXAMPLE 74 4-[5-(1,2-Dithiolan-3-yl)pentanoylamino]butanoic acid(Compound No. 1-1275) ##STR88##

The reaction was effected as described in Example 49, but using 0.65 gof methyl 4-[5-(1,2-dithiolan-3yl)pentanoylamino]butanoate (prepared asdescribed in Example 73), 13 ml of methanol and a 1N aqueous solution ofsodium hydroxide. The solvent was removed from the reaction mixture bydistillation under reduced pressure. Water was added to the residue.After neutralisation with 2N aqeous hydrochloric acid, the resultingmixture was extracted with ethyl acetate. The extract was washed with asaturated aqueous solution of sodium chloride and then dried overanhydrous sodium sulfate. Ethyl acetate was removed from the extract bydistillation under reduced pressure. The residue was recrystallized fromethyl acetate, to give 0.28 g of the title compound as yellow crystals,melting at 56 to 58° C.

EXAMPLE 75 Methyl 4-{3-[4-(1,2-dithiolan-3-yl)buty]ureido}butanoate(Compound No. 1-1276 methyl ester) ##STR89##

The reaction was effected as described in Example 46, but using 1.00 gof D,L-α-lipoic acid, 20 ml of anhydrous toluene, 1.48 ml oftriethylamine, 1.15 ml of diphenylphosphoryl azide and 0.74 g of methyl4-aminobutanoate hydrochloride. The solvent was removed from thereaction mixture by distillation under reduced pressure. Water was addedto the residue, after which it was extracted with ethyl acetate. Theextract was washed with a saturated aqueous solution of sodium chlorideand then dried over anhydrous sodium sulfate. Ethyl acetate was removedfrom the extract by distillation under reduced pressure. The residue wassubjected to silica gel column chromatography, using ethyl acetate aseluent. The ethyl acetate was removed from the eluate so obtained bydistillation under reduced pressure, to give 1.18 g of the titlecompound as yellow crystals, melting at 63 to 70° C.

EXAMPLE 76 N-[5-(1,2-Dithiolan-3-yl)pentyl]oxalamic acid (Compound No.1-2589) ##STR90##

The reaction was effected as described in Example 49, but using 92 mg ofmethyl N-[5-(1,2-dithiolan-3-yl)pentyl]oxcalamidate (prepared asdescribed in Example 65), 4 ml of methanol, 1 ml of tetrahydrofuran and0.6 ml of a 1N aqueous solution of sodium hydroxide. The solvent wasremoved from the reaction mixture by distillation under reducedpressure. Water was added to the residue. The resulting mixture wasneutralized by the addition of 2N aqueous hydrochloric acid, after whichit was extracted with ethyl acetate. The extract was washed with asaturated aqueous solution of sodium chloride and then dried overanhydrous sodium sulfate. Ethyl acetate was removed from the extract bydistillation under reduced pressure. The residue was dissolved indioxane, after which it was lyophilised, to give 64 mg of the titlecompound as a pale yellow amorphous substrate, melting at 75 to 79° C.

EXAMPLE 77 Methyl N-[5-(1,2-dithiolan-3-yl)pentyl]succinamidate(Compound No. 1-1970 methyl ester) ##STR91##

0.25 ml of a hexane solution containing 2.0 M of(trimethylsilyl)diazomethane was added dropwise to a mixture of 89 mg ofN-[5-(1,2-dithiolan-3-yl)pentyl]-succinamic acid, 1 ml of methanol and1.5 ml of toluene, and then the mixture was stirred at room temperaturefor 30 minutes. At the end of this time, the solvent was removed fromthe reaction mixture by distillation under reduced pressure. Theresulting residue was subjected to silica gel column chromatography,using 1:1 and 1:0 by volume mixtures of ethyl acetate and hexane aseluent. Ethyl acetate and hexane were removed from the eluate soobtained by distillation under reduced pressure. The resulting residuewas dissolved in dioxane, after which it was lyophilised, to give 77 mgof the title compound as a pale yellow amorphous substance, melting at46 to 48° C.

EXAMPLE 78 Methyl 4-[5-(1,2-dithiolan-3-yl)pentylcarbamoyl]butanoate(Compound No. 1-2577 methyl ester) ##STR92##

The reaction was effected as described in Example 77, but using 68 mg of4-[5-(1,2-dithiolan-3-yl)pentylcarbamoyl]butanoic acid (prepared asdescribed in Example 67), 1 ml of methanol, 1 ml of toluene and 0.40 mlof a hexane solution containing 2.0M of (trimethylsilyl)diazomethane.The solvent was then removed from the reaction mixture by distillationunder reduced pressure. The residue was subjected to silica gel columnchromatography, using 3:1 and 1:0 by volume mixtures of ethyl acetateand hexane as eluent. The solvent was removed from the eluate soobtained by distillation under reduced pressure. The residue wasdissolved in dioxane, after which it was lyophilised, to give 62 mg ofthe title compound as a pale yellow amorphous substrate, melting at 69to 71° C.

EXAMPLE 79 Ethyl{N-[5-(1,2-dithiolan-3-yl)pentanoyl]-N-methylamino}acetate (Compound No.1-2520 ethyl ester) ##STR93##

The reaction was effected as described in Example 47, but using 500 mgof D,L-α-lipoic acid, 10 ml of anhydrous dimethylformamide, 422 mg ofN,N'-carbonyldiimidazole, 0.36 ml of triethylamine and 399 mg ofsarcosine ethyl ester hydrochloride. The solvent was removed from thereaction mixture by distillation under reduced pressure. Water was addedto the residue, after which it was extracted with ethyl acetate. Theextract was washed with a saturated aqueous solution of sodium chlorideand then dried over anhydrous sodium sulfate. Ethyl acetate was removedfrom the extract by distillation under reduced pressure, and the residuewas subjected to silica gel column chromatography, using a 2:1 by volumemixture of ethyl acetate and hexane as eluent. The solvent was removedfrom the eluate by distillation under reduced pressure. The residue wasdissolved in dioxane, after which it was lyophilised, to give 558 mg ofthe title compound as a yellow oil having an Rf value of 0.39 (silicagel thin layer chromatography; using a 2:1 by volume mixture of ethylacetate and hexane as the developing solvent).

EXAMPLE 80 Methyl4-{N-[5-(1,2-dithiolan-3-yl)pentanoyl]-N-methylamino}butanoate (CompoundNo. 1-2669 methyl ester) ##STR94##

The reaction was effected as described in Example 47, but using 500 mgof D,L-α-lipoic acid, 10 ml of anhydrous dimethylformamide, 422 mg ofN,N'-carbonyldiimidazole, 0.36 ml of triethylamine and 486 mg of methyl4-(methylamino)butanoate hydrochloride. The solvent was removed from thereaction mixture by distillation under reduced pressure. Water was addedto the residue, after which it was extracted with ethyl acetate. Theextract was washed with a saturated aqueous solution of sodium chlorideand then dried over anhydrous sodium sulfate. Ethyl acetate was removedfrom the extract by distillation under reduced pressure, and the residuewas subjected to silica gel column chromatography, using 2:1 and 4:1 byvolume mixtures of ethyl acetate and hexane as eluent, followed byreverse phase preparative silica gel column chromatography, using 2:3and 9:11 by volume mixtures of acetonitrile and water as eluent.Acetonitrile was removed from the eluate so obtained by distillationunder reduced pressure, and the residue was extracted with ethylacetate. The extract was washed with a saturated aqueous solution ofsodium chloride and then dried over anhydrous sodium sulfate. Ethylacetate was removed from the extract by distillation under reducedpressure. The residue was then dissolved in dioxane, after which it waslyophilised, to give 229 mg of the title compound as a yellow oil havingan Rf value of 0.37 (silica gel thin layer chromatography; using a 4:1by volume mixture of ethyl acetate and hexane developing solvent).

EXAMPLE 81 2-[4-(1,2-Dioxothiazolidin-5-ylmethyl)phenoxymethyl]-2,5,7,8-tetramethylchroman-6-yl5-(1,2-dithiolan-3-yl)pentanoate ##STR95##

0.36 ml of triethylamine and then 0.25 ml of ethyl chloroformate wereadded dropwise to 10 ml of solution of 500 mg of D,L-α-lipoic acid inanhydrous dimethylformamide, whilst ice-cooling, and the mixture wasstirred at room temperature for 2 hours. At the end of this time, 1.06 gof5-[4-(2,5,7,8-tetramethylchroman-2-ylmethoxy)benzyl]thiazolidine-2,4-dionewere added to the reaction solution, whilst ice-cooling, and the mixturewas stirred at room temperature for 5 hours, after which it was left tostand at room temperature overnight. The mixture was then stirred on anoil bath at 50° C. for 1 hour, and then the solvent was removed from thereaction mixture by evaporation under reduced pressure. Water was addedto the residue, and the mixture was extracted with ethyl acetate. Theextraction solution was washed with a standard aqueous solution ofsodium chloride and dried over anhydrous sodium sulfate. The ethylacetate was removed from the extraction solution by evaporation underreduced pressure, and the residue was subjected to silica gel columnchromatography, using a 3:2 by volume mixture of ethyl acetate andhexane as the eluent. The residue was then subjected to reverse phasepreparative silica gel column chromatography, using 3:1 and 4:1 byvolume mixtures of acetonitrile and water as eluent. The acetonitrilewas removed from the solution by evaporation under reduced pressure,after which the residue was extracted with ethyl acetate. The extractionsolution was washed with a saturated aqueous solution of sodium chlorideand dried over anhydrous sodium sulfate. The ethyl acetate was removedfrom the extraction solution by evaporation under reduced pressure, andthe residue was dissolved in dioxane and then lyophilised, to obtain0.57 g of the title compound as a yellow oil having an Rf value of 0.42(silica gel thin layer chromatography; using a 1:2 by volume mixture ofethyl acetate and hexane as developing solvent).

EXAMPLE 822-(3,4-Dibenzyloxy-5-oxo-2,5-dihydrofuran-2-yl)-2-hydroxyethyl5-(1,2-dithiolan-3-yl)pentanoate ##STR96##

276 mg of N,N'-carbonyldiimidazole were added, whilst ice-cooling, to 6ml of a solution of 300 mg of D,L-α-lipoic acid in anhydrousdimethylformamide and the mixture was stirred at room temperature for 1hour and 30 minutes. At the end of this time, 0.24 ml of triethylamineand 536 mg of 2,3-O-dibenzylascorbic acid were added, whilstice-cooling, to the reaction solution, and the mixture was stirred atroom temperature for 1 hour, after which the reaction mixture was leftto stand at room temperature for 2 days. The solvent was then removedfrom the reaction mixture by evaporation under reduced pressure. Waterwas added to the residue, and the mixture was extracted with ethylacetate. The extraction solution was washed with a saturated aqueoussolution of sodium chloride and dried over anhydrous sodium sulfate. Theethyl acetate was removed from the extraction solution by evaporationunder reduced pressure, and the residue was subjected to silica gelcolumn chromatography, using 1:3 and 1:1 by volume mixtures of ethylacetate and hexane as the eluent. The residue was then subjected toreverse phase preparative silica gel column chromatography, using11:9,3:2 and 13:7 by volume mixtures of acetonitrile and water aseluent, and the acetonitrile was removed form the solution byevaporation. under reduced pressure, after which the residue wasextracted with ethyl acetate. The extraction solution was washed with asaturated aqueous solution of sodium chloride and dried over anhydroussodium sulfate. The ethyl acetate was removed from the extractionsolution by evaporation under reduced pressure, and the residue wasdissolved in dioxane and then lyophilised, to obtain 321 mg of the titlecompound as a yellow oil having an Rf value of 0.34 (silica gel thinlayer chromatography; using a 1:2 by volume mixture of ethyl acetate andhexane as developing solvent).

EXAMPLE 83 5-(1,2-Dithiolan-3-yl)-1-(imidazol-1-yl)pentan-1-one##STR97##

0.86 g of N,N'-carbonyldiimidazole was added, whilst ice-cooling, to 20ml of a solution of 1.00 g of D,L-α-lipoic acid in anhydrousdimethylformamide, and the mixture was stirred at room temperature for 1hour. At the end of this time, 311 mg of chloromethanesulfonamide and104 mg of sodium hydride (as a 55% w/w dispersion in mineral oil) wereadded, whilst ice-cooling, to the reaction solution, and the mixture wasstirred at room temperature for 1 hour. The reaction mixture was thenleft to stand at room temperature overnight, after which the solvent wasremoved from the reaction mixture by evaporation under reduced pressure.Water was added to the residue and the mixture was neutralized by theaddition of 2N aqueous hydrochloric acid, after which it was extractedwith ethyl acetate. The extraction solution was washed with a saturatedaqueous solution of sodium chloride and dried over anhydrous sodiumsulfate. The ethyl acetate was removed from the extraction solution byevaporation under reduced pressure, and the residue was subjected tosilica gel column chromatography, using 2:1, 4:1 and 1:0 by volumemixtures of ethyl acetate and hexane as the eluent. The residue was thensubjected to reverse phase preparative silica gel column chromatography,using 2:3 and 1:1 by volume mixtures of acetonitrile and water aseluent, and the acetonitrile was removed from the solution byevaporation under reduced pressure, after which the residue wasextracted with ethyl acetate. The extraction solution was washed with asaturated aqueous solution of sodium chloride and dried over anhydroussodium sulfate. The ethyl acetate was removed from the extractionsolution by evaporation under reduced pressure, and the residue wasdissolved in dioxane and then lyophilised, to obtain 245 mg of the titlecompound as a pale yellow amorphous substance, melting at 37 to 39° C.

EXAMPLE 84 t-Butyl4-[5-(1,2-dithiolan-3-yl)pentanoyl]piperazine-1-carboxylate (CompoundNo. 1-1131 t-butoxycarbonyl derivative) ##STR98##

The reaction was carried out as described in Example 43, but using 500mg of D,L-α-lipoic acid, 10 ml of anhydrous dimethylformamide, 442 mg ofN,N'-carbonyldiimidazole and 484 mg of N-t-butoxycarbonylpiperazine. Thesolvent was removed from the reaction mixture by evaporation underreduced pressure, and water was added to the residue, after which it wasextracted with ethyl acetate. The extraction solution was washed with asaturated aqueous solution of sodium chloride and dried over anhydroussodium sulfate. The ethyl acetate was removed from the extractionsolution by evaporation under reduced pressure, and the residue wassubjected to silica gel column chromatography, using 2:1 and 1:0 byvolume mixtures of ethyl acetate and hexane as the eluent. The residuewas dissolved in dioxane and then lyophilised, to obtain 520 mg of thetitle compound as a pale yellow amorphous substance, melting at 70 to71° C.

EXAMPLE 85 5-(1,2-Dithiolan-3-yl)-1-(piperazin-1-one hydrochloride(Compound No. 1-1131 hydrochloride) ##STR99##

3 ml of a 4N solution of hydrogen chloride in ethyl acetate were addeddropwise to 5 ml of a solution of 260 mg of t-butyl4-[5-(1,2-dithiolan-3-yl)pentanoyl]-piperazine-1-carboxylate (preparedas described in Example 84) in ethyl acetate, and the mixture wasstirred at room temperature for 3 hours. The crystals which precipitatedwere then collected by filtration, to obtain 217 mg of the titlecompound as a pale yellow powder, melting at 84 to 86° C.

EXAMPLE 86 Thiazolidine-3-carboxylic acid[4-(1,2-dithiolan-3yl)butyl]amide (Compound No. 1-1260) ##STR100##

The reaction was carried out as described in Example 44, but using 500mg of D,L-α-lipoic acid, 10 ml of anhydrous toluene, 0.36 ml oftriethylamine, 0.56 ml of diphenylphosphoryl azide and 0.20 ml ofthiazolidine. The solvent was removed from the reaction mixture byevaporation under reduced pressure, and water was added to the residue,after which it was extracted with ethyl acetate. The extraction solutionwas washed with a saturated aqueous solution of sodium chloride anddried over anhydrous sodium sulfate. The ethyl acetate was removed fromthe extraction solution by evaporation under reduced pressure, and theresidue was subjected to silica gel. column chromatography using 2:1 and1:0 by volume mixtures of ethyl acetate and hexane as the eluent. Thesolvent was removed from the eluate by evaporation under reducedpressure, and the residue was recrystallized from a 1:1 by volumemixture of ethyl acetate and hexane, to obtain 386 mg of the titlecompound as yellow crystals, melting at 76 to 77° C.

EXAMPLE 87 5-(1,2-Dithiolan-3-yl)pentanoic acid(1-methyl-2-nitroxyethyl)amide (Compound No. 1-2665 nitrate) ##STR101##

The reaction was carried out as described in Example 47, but using 300mg of D,L-α-lipoic acid, 9 ml of anhydrous dimethylformamide, 259 mg ofN,N'-carbonyldiimidazole, 0.22 ml of triethylamine and 251 mg of1-methyl-2-nitroxyethylamine hydrochloride. The solvent was removed fromthe reaction mixture by evaporation under reduced pressure, and waterwas added to the residue, after which it was extracted with ethylacetate. The extraction solution was washed with a saturated aqueoussolution of sodium chloride and dried over anhydrous sodium sulfate. Theethyl acetate was removed from the extraction solution by evaporationunder reduced pressure, and the residue was subjected to silica gelcolumn chromatography, using 3:2 and 2:1 by volume mixtures of ethylacetate and hexane as the element. The residue was then subjected toreverse phase preparative silica gel column chromatography, using 3:7,and 2:3 and 7:3 by volume mixtures of acetonitrile and water as eluent,and the acetonitrile was removed from the solution by evaporation underreduced pressure, after which the residue was extracted with ethylacetate. The extraction solution was washed with a saturated aqueoussolution of sodium chloride and dried over anhydrous sodium sulfate. Theethyl acetate was removed from the extraction solution by evaporationunder reduced pressure, and the residue was dissolved in a dioxane andthen lyophilised, to obtain 119 mg of the title compound as a yellow oilhaving an Rf value of 0.39 (silica gel thin layer chromatography; usinga 2:1 by volume mixture of ethyl acetate and hexane as developingsolvent).

EXAMPLE 88 1-[4-(1,2-Dithiolan-3-yl)butyl]-3-(2-nitroxyethyl)urea(Compound No. 1-2661 nitrate) ##STR102##

The reaction was carried out as described in Example 46, but using 500mg of D,L-α-lipoic acid, 10 ml of anhydrous toluene, 0.72 ml oftriethylamine, 0.56 ml of diphenylphosphoryl azide, 10 ml of anhydrousdimethylformamide and 342 mg of 2-nitroxyethylamine hydrochloride. Thesolvent was removed from the reaction mixture by evaporation underreduced pressure, and water was added to the residue, after which it wasextracted with ethyl acetate. The extraction solution was washed with asaturated aqueous solution of sodium chloride and dried over anhydroussodium sulfate. The ethyl acetate was removed from the extractionsolution by evaporation under reduced pressure, and the residue wassubjected to silica gel column chromatography, using 2:1 and 1:0 byvolume mixtures of ethyl acetate and hexane as the eluent. The solventwas removed from the eluate by evaporation under reduced pressure, andthe residue was recrystallized from a 1:2 by volume mixture of ethylacetate and hexane, to obtain 58 mg of the title compound as a paleyellow powder having an Rf value of 0.31 (silica gel thin layerchromatography; using a 2:1 by volume mixture of ethyl acetate andhexane as developing solvent).

EXAMPLE 89 3-(1,2-Dithiolan-3-yl)propionic acid ##STR103##

1.3 ml of 2N aqueous hydrochloric acid were added to a solution of 500mg of 4,6-dithioxyhexanoic acid in 5 ml of a 1N aqueous solution ofsodium hydroxide. 5 drops of a 1% w/v aqueous solution of ferricchloride were then added dropwise to the reaction solution, and theresulting mixture was stirred at room temperature for 1 hour while airwas blown through the mixture. Water was then added to the reactionsolution, which was then washed with ethyl acetate. The aqueous layerwas neutralized by the addition of 2N aqueous hydrochloric acid and thenextracted with ethyl acetate. The extraction solution was washed with asaturated aqueous solution of sodium chloride and dried over anhydroussodium sulfate. The ethyl acetate was removed from the extractionsolution by evaporation under reduced pressure, and the residue wasdissolved in dioxane and then lyophilised, to obtain 388 mg of the titlecompound as a yellow oil having an Rf value of 0.59 (silica gel thinlayer chromatography; using a 2:1 by volume of ethyl acetate and hexaneas developing solvent).

EXAMPLE 90 2-[5-(1,2-Dithiolan-3-yl)pentanoylamino]acetamide (CompoundNo. 1-46 amide) ##STR104##

The reaction was carried out as described in Example 47, but using 500mg of D,L-α-lipoic acid, 10 ml of anhydrous dimethylformamide, 422 mg ofN,N'-carbonyldiimidazole, 0.36 ml of triethylamine and 265 mg ofglycinamide. The solvent was removed from the reaction mixture byevaporation under reduced pressure, and water was added to the residue,after which it was extracted with ethyl acetate. The extraction solutionwas washed with a saturated aqueous solution of sodium chloride anddried over anhydrous sodium sulfate. The ethyl acetate was removed fromthe extraction solution by evaporation under reduced pressure, and thecrystals which precipitated were collected by filtration, to obtain 330mg of the title compound as yellow crystals, melting at 105 to 108° C.

EXAMPLE 91 2-{3-[4-(1,2-Dithiolan-3-yl)butyl]ureido}acetamide (CompoundNo. 1-738 amide) ##STR105##

The reaction was carried out as described in Example 46, but using 500mg of D,L-α-lipoic acid, 10 ml of anhydrous toluene, 0.56 ml oftriethylamine, 0.72 ml of diphenylphosphoryl azide, 10 ml of anhydrousdimethylformamide and 265 mg of glycinamide hydrochloride. The solventwas removed from the reaction mixture by evaporation under reducedpressure, and water was added to the residue, after which it wasextracted with ethyl acetate. The extraction solution was washed with asaturated aqueous solution of sodium chloride and dried over anhydroussodium sulfate. The ethyl acetate was removed from the extractionsolution by evaporation under reduced pressure, and the residue wasrecrystallized from ethyl acetate, to obtain 149 mg of the titlecompound as yellow powder, melting at 141 to 143° C.

EXAMPLE 92 1-(Indolin-1-yl)-5-(1,2-dithiolan-3-yl)pentan-1-one (CompoundNo. 1-2674) ##STR106##

The reaction was carried out as described in Example 43, but using 1.00g of D,L-α-lipoic acid, 30 ml of anhydrous dimethylformamide, 0.86 g ofN,N'-carbonyldiimidazole, 0.73 ml of triethylamine and 1.13 g of methylindoline-2-carboxylate hydrochloride. The solvent was removed from thereaction mixture by evaporation under reduced pressure, and water wasadded to the residue, after which it was extracted with ethyl acetate.The extraction solution was washed with a saturated aqueous solution ofsodium chloride and dried over anhydrous sodium sulfate. The ethylacetate was removed from the extraction solution by evaporation underreduced pressure, and the residue was subjected to silica gel columnchromatography, using 1:4 and 1:2 by volume mixtures of ethyl acetateand hexane as the eluent. The residue was then subjected to reversephase preparative silica gel column chromatography, using a 3:2 byvolume mixture of acetonitrile and water as eluent, and the acetonitrilewas removed from the solution by evaporation under reduced pressure,after which the residue was extracted with ethyl acetate. The extractionsolution was washed with a saturated aqueous solution of sodium chlorideand dried over anhydrous sodium sulfate. The ethyl acetate was removedfrom the extraction solution by evaporation under reduced pressure, andthe residue was dissolved in dioxane and then lyophilised, to obtain0.84 g of the title compound as a pale yellow powder, melting at 65 to66° C.

EXAMPLE 93 Methyl1-[4-(1,2-dithiolan-3-yl)butylcarbamoyl]indoline-2-carboxylate (CompoundNo. 1-2676 methyl ester) ##STR107##

The reaction was carried out as described in Example 44, but using 1.00g of D,L-α-lipoic acid, 25 ml of anhydrous toluene, 0.73 ml oftriethylamine, 1.14 ml of diphenylphosphoryl azide and 0.94 g of methylindoline-2-carboxylate. The reaction solution was washed with water, andthe toluene layer was separated and washed with a saturated aqueoussolution of sodium chloride and dried over anhydrous sodium sulfate. Thetoluene was removed from the extraction solution by evaporation underreduced pressure, and the residue was subjected to silica gel columnchromatography, using 1:2, 1:1 and 2:1 by volume mixtures of ethylacetate and hexane as the eluent. The solvent was removed from ethylacetate, to obtain 485 mg of the title compound as yellow crystals,melting at 86 to 89° C.

EXAMPLE 94 1-[4-(1,2-Dithiolan-3-yl)butylcarbamoyl]indoline-2-carboxylicacid (Compound No. 1-2676) ##STR108##

The reaction was carried out as described in Example 48, but using 200mg of methyl1-[4-(1,2-dithiolan-3-yl)butylcarbamoyl]indoline-2-carboxylate (preparedas described in Example 93), 4 ml of methanol, 2 ml of tetrahydrofuranand 1.0 ml of a 1N aqueous solution of sodium hydroxide. The solvent wasremoved from the reaction mixture by evaporation under reduced pressure,and water was added to the residue. The mixture was neutralized by theaddition of 2N aqueous hydrochloride acid and extracted with ethylacetate. The extraction solution was washed with a saturated aqueoussolution of sodium chloride and dried over anhydrous sodium sulfate. Theethyl acetate was removed from the extraction solution by evaporationunder reduced pressure, and the residue was dissolved in dioxane andthen lyophilised, to obtain 98 mg of the title compound as a pale yellowamorphous substance having an Rf value of 0.12 (silica gel thin layerchromatography, using a 2:1 by volume mixture of ethyl acetate andhexane as developing solvent).

EXAMPLE 95 Methyl 3-[3-(1,2-dithiolan-3-yl)propionylamino]propionate##STR109##

5 ml of anhydrous tetrahydrofuran were added to 6 ml of a mixture of 2.5mmol of 3-(1,2-dithiolan-3-yl)propionic acid in a mixture of ethylacetate and dimethylformamide. 0.6 ml of triethylamine, 349 mg ofβ-alanine methyl ester hydrochloride and 0.38 ml of diethylcyanophosphate were added to the reaction solution, whilst ice-cooling,and the resulting mixture was stirred, whilst ice-cooling for 1 hour. Atthe end of this time, the reaction mixture was stirred at roomtemperature for 30 minutes, and then the solvent was removed from thereaction mixture by evaporation under reduced pressure. Water was addedto the residue, and the mixture was extracted with ethyl acetate. Theextraction solution was washed with a saturated aqueous solution ofsodium chloride and dried over anhydrous sodium sulfate. The ethylacetate was removed from the extraction solution by evaporation underreduced pressure, and the residue was subjected to silica gel columnchromatography, using 2:1,3:1 and 1:0 by volume mixtures of ethylacetate and hexane as the eluent. The residue was then subjected toreverse phase preparative silica gel column chromatography, using a 2:3by volume mixture of acetonitrile and water as a eluent, and theacetonitrile was removed from the solution by evaporation under reducedpressure, after which the residue was extracted with ethyl acetate. Theextraction solution was washed with a saturated aqueous solution ofsodium chloride and dried over anhydrous sodium sulfate. The ethylacetate was removed from the extraction solution by evaporation underreduced pressure, and the residue was dissolved in dioxane and thenlyoiphilised, to obtain 229 mg of the title compound as a yellow oilhaving an Rf value of 0.24 (silica gel thin layer chromatography; usinga 3:1 by volume mixture of ethyl acetate and hexane as developingsolvent).

EXAMPLE 96 1,2-Dithiolane-4-carboxylic acid ##STR110##

40 ml of 5N aqueous hydrochloric acid were added to 20 ml of a solutionof 3.60 g of methyl (1,3-diacetylthio)propyl-2-carboxylic in methanol,and the mixture was heated under reflux for 5 hours and 30 minutes. Atthe end of this time, the reaction mixture was left to stand at roomtemperature overnight, and then the solvent was removed from thereaction mixture by evaporation under reduced pressure. Water was addedto the residue, and the mixture was extracted with ethyl acetate. Theextraction solution was washed with a dilute aqueous solution of sodiumhydrogencarbonate, and then with a saturated aqueous solution of sodiumchloride, after which it was dried over anhydrous sodium sulfate. Theethyl acetate was removed from the extraction solution by evaporationunder reduced pressure, and 150 ml of a saturated aqueous solution ofsodium hydrogencarbonate and a catalytic amount of ferric chloride 6hydrate were added to the residue, and then the mixture was stirred atroom temperature for 8 hours. The reaction mixture was then left tostand at room temperature overnight, after which the solvent was removedfrom the reaction mixture by evaporation under reduced pressure. Waterwas added to the residue, and the resulting mixture was washed withethyl acetate. The pH of the aqueous layer was adjusted to a value of 2by the addition of aqueous hydrochloric acid, and the mixture wasextracted with ethyl acetate. The extraction solution was washed with asaturated aqueous solution of sodium chloride and dried over anhydroussodium sulfate. The ethyl acetate was removed from the extractionsolution by evaporation under reduced pressure, and the residue wasdissolved in dioxane and then lyophilised, to obtain 0.25 g of the titlecompound as yellow crystals having an Rf value of 0.56 (silica gel thinlayer chromatography; using a 5:1 by volume mixture of ethyl acetate andmethanol as developing solvent).

EXAMPLE 97 Methyl 1,2-dithiolan-4-ylcarbonylaminoacetate ##STR111##

5 ml of anhydrous tetrahydrofuran, 1.01 ml of triethylamine and 398 mgof glycine methyl ester hydrochloride were added to 5 ml of a solutionof 3.3 mmol of 1,2-dithiolane-4-carboxylic acid (prepared as describedin Example 96) in anhydrous dimethylformamide, and 0.55 ml of diethylcyanophosphate was then added to the resulting mixture, whilst theice-cooling, after which the mixture was stirred at room temperature for5 hours. At the end of this time, the reaction mixture was left to standat room temperature overnight, after which the solvent was removed fromthe reaction mixture by evaporation under reduced pressure. Water wasadded to the residue, and the mixture was extracted with ethyl acetate.The extraction solution was washed with a saturated aqueous solution ofsodium chloride and dried over anhydrous sodium sulfate. The ethylacetate was removed from the extraction solution by evaporation underreduced pressure, and the residue was subjected to silica gel columnchromatography, using a 2:1 by volume mixture of ethyl acetate andhexane as the eluent. The solvent was then removed from the eluatesolution by evaporation under reduced pressure, and the residue wasrecrystallized from a 1:2 by volume mixture of ethyl acetate and hexane,to obtain 54 mg of the title compound as pale yellow crystals, meltingat 73 to 75° C.

EXAMPLE 98 Methyl 3-(1,2-dithiolan-4-ylcarbonyl)aminopropionate##STR112##

The reaction was carried out as described in Example 97, but using 5 mlof a solution of 3.3 mmol of 1,2-dithiolane-4-carboxylic acid (preparedas described in Example 96) in anhydrous dimethylformamide, 5 ml ofanhydrous tetrahydrofuran, 1.01 ml of triethylamine, 502 mg of β-alaninemethyl ester hydrochloride and 0.55 ml of diethyl cyanophosphate. Thesolvent was removed from the reaction mixture by evaporation underreduced pressure, and water was added to the residue, after which it wasextracted with ethyl acetate. The extraction solution was washed with asaturated aqueous solution of sodium chloride and dried over anhydroussodium sulfate. The ethyl acetate was removed from the extractionsolution by evaporation under reduced pressure, and the residue wassubjected to silica gel column chromatography, using a 2:1 by volumemixture of ethyl acetate and hexane as the eluent. The solvent wasremoved from the eluate solution by evaporation under reduced pressure,and the residue was recrystallized from a 2:1 by volume mixture of ethylacetate and hexane, to obtain 73 mg of the title compound as pale yellowcrystals having an Rf value of 0.41 (silica gel thin layerchromatography; using a 2:1 by volume mixture of ethyl acetate andhexane as developing solvent).

EXAMPLE 99 C-Chloro-N-[5-(1,2-dithiolan-3-yl)pentyl]methanesulfonamide(Compound No. 1-2473) ##STR113##

The reaction was carried out as described in Example 60, but using 3 mlof a solution of 1.6 mmol of2-[5-(1,2-dithiolan-3-yl)pentyl]isoindoline-1,3-dione (prepared asdescribed in Example 58) in toluene, 2 ml of methanol, 2 ml ofbutylamine, 5 ml of anhydrous tetrahydrofuran, 0.33 ml of triethylamineand 0.21 ml of chloromethanesulfonyl chloride. The solvent was removedfrom the reaction mixture by evaporation under reduced pressure, andwater was added to the residue, after which it was extracted with ethylacetate. The extraction solution was washed with a saturated aqueoussolution of sodium chloride and dried over anhydrous sodium sulfate. Theethyl acetate was removed from the extraction solution by evaporationunder reduced pressure, and the residue was subjected to silica gelcolumn chromatography, using 2:5 and 2:3 by volume mixtures of ethylacetate and hexane as the eluent. The ethyl acetate was removed from theeluate solution by evaporation under reduced pressure, and the residuewas dissolved in dioxane and then lyophilised, to obtain 42 mg of thetitle compound as a brown oil having an Rf value of 0.29 (silica gelthin layer chromatography; using a 2:5 by volume mixture of ethylacetate and hexane as developing solvent).

EXAMPLE 100 N-[5-(1,2-Dithiolan-3-yl)pentyl]benzamide (Compound No.1-1923) ##STR114##

2 ml of methanol and 2 ml of butylamine were added to 3 ml of a solutionof 1.6 mmol of 2-[5-(1,2-dithiolan-3-yl)pentyl]isoindoline-1,3-dione(prepared as described in Example 58) in toluene, and the mixture wasstirred at room temperature for 1 hour. The reaction mixture was thenleft to stand at room temperature for 2 days, after which the solventwas removed from the reaction mixture by evaporation under reducedpressure. Water was added to the residue, and the mixture was extractedwith ethyl acetate. The extraction solution was washed with saturatedaqueous solution of sodium chloride and dried over anhydrous sodiumsulfate. The ethyl acetate was removed from the extraction solution byevaporation under reduced pressure, and 5 ml of anhydroustetrahydrofuran, 0.33 ml of triethylamine and 0.28 ml of benxoylchloride were added to the residue. The mixture was then stirred at roomtemperature for 6 hours. At the end of this time, the solvent wasremoved from the reaction mixture by evaporation under reduced pressure,and water was added to the residue, after which it was extracted withethyl acetate. The extraction solution was washed with a saturatedaqueous solution of sodium chloride and dried over anhydrous sodiumsulfate. The ethyl acetate was removed from the extraction solution byevaporation under reduced pressure, and the residue was subjected tosilica gel column chromatography, using 1:8, 1:4 and 1:2 by volumemixtures of ethyl acetate and hexane as the eluent. The residue was thensubjected to reverse phase preparative silica gel column chromatography,using 2:3 and 1:1 by volume mixtures of acetonitrile and water waseluent, and the acetonitrile was removed from the solution byevaporation under reduced pressure, after which the residue wasextracted with ethyl acetate. The extraction solution was washed with asaturated aqueous solution of sodium chloride and dried over anhydroussodium sulfate. The ethyl acetate was removed from the extractionsolution by evaporation under reduced pressure, and the residue wasdissolved in dioxane and then lyophilised, to obtain 56 mg of the titlecompound as a yellow amorphous substance, melting at 58 to 59° C.

EXAMPLE 101 N-[5-(1,2-Dithiolan-3-yl)pentyl]nicotinamide (Compound No.1-1991) ##STR115##

The reaction was carried out as described in Example 100, but using 3 mlof a solution of 1.6 mmol of2-[5-(1,2-dithiolan-3-yl)pentyl]isoindoline-1,3-dione (prepared asdescribed in Example 58) in toluene, 2 ml of methanol, 2 ml ofbutylamine, 5 ml of anhydrous tetrahydrofuran, 0.33 ml of triethylamineand 427 mg of nicotinoyl chloride hydrochloride. The solvent was removedfrom the reaction mixture by evaporation under reduced pressure, andwater was added to the residue, after which it was extracted with ethylacetate. The extraction solution was washed with a saturated aqueoussolution of sodium chloride and dried over anhydrous sodium sulfate. Theethyl acetate was removed from the extraction solution by evaporationunder reduced pressure, and the residue was subjected to silica gelcolumn chromatography, using 3:1 and 1:0 by volume mixtures of ethylacetate and hexane and a 20:1 by volume mixture of ethyl acetate andmethanol as the eluent. The solvent was removed from the eluate byevaporation under reduced pressure, and the residue was dissolved indioxane and then lyophilised, to obtain 156 mg of the title compound asa yellow amorphous substance, melting at 41 to 44° C.

EXAMPLE 102 N-Butyl-N'-[5-(1,2-dithiolan-3-yl)pentyl]phthalamide(Compound No. 1-1936 N-butylamide) ##STR116## (a) 4 ml of methanol and 4ml of butylamine were added to 6 ml of a solution of 3.0 mmol of2-[5-(1,2-dithiolan-3-yl)pentyl]isoindoline-1,3-dione (prepared asdescribed in Example 58) in toluene, and the mixture was stirred at roomtemperature for 1 hour. The reaction mixture was then left to stand atroom temperature overnight, after which the solvent was removed from thereaction mixture by evaporation under reduced pressure. Water was addedto the residue, and the mixture was extracted with ethyl acetate. Theextraction solution was washed with a saturated aqueous solution ofsodium chloride and dried over anhydrous sodium sulfate, and then theethyl acetate was removed from the extraction solution by evaporationunder reduced pressure, to give a residue.

(b) 584 mg of N,N'-carbonyldiimidazole were added to 5 ml of a solutionof 770 mg of N-t-butoxycarbonylthiazolidine in anhydrousdimethylformamide, and the mixture was stirred at room temperature for 3hours. A solution of three residue prepared as described in step (a)above in 3 ml of anhydrous dimethylformamide was then added to thereaction mixture, whilst ice-cooling, and the resulting mixture wasstirred at room temperature for 5 hours and 30 minutes. The solvent wasthen removed from the reaction mixture by evaporation under reducedpressure, and water was added to the residue, after which it wasextracted with ethyl acetate. The extraction solution was washed with asaturated aqueous solution of sodium chloride and dried over anhydroussodium sulfate. The ethyl acetate was removed from the extractionsolution by evaporation under reduced pressure, and the residue wassubjected to reverse phase preparative silica gel column chromatography,using a 1:1 by volume mixture of acetonitrile and water as eluent. Theacetonitrile was removed from the solution by evaporation under reducedpressure, and the precipitated insolubles were collected by filtration,to obtain 118 mg of the title compound as a white powder having an Rfvalue of 0.44 (silica gel thin layer chromatography; using a 1:1 byvolume mixture of ethyl acetate and hexane as developing solvent).

EXAMPLE 103N-[4-(1,2-Dithiolan-3-yl)butyl]-N'-(2-hydroxy-1-methylethyl)urea(Compound No. 1-2667) ##STR117##

The reaction was carried out as described in Example 46, but using 1.00g of D,L-α-lipoic acid, 25 ml of anhydrous toluene, 0.74 ml oftriethylamine, 1.15 ml of diphenylphosphoryl azide and 0.39 ml ofD,L-alaninol. The solvent was removed from the reaction mixture byevaporation under reduced pressure, and water was added to the residue,after which it was extracted with ethyl acetate. The extraction solutionwas washed with a saturated aqueous solution of sodium chloride anddried over anhydrous sodium sulfate. The ethyl acetate was removed fromthe extraction solution by evaporation under reduced pressure, and theresidue was subjected to silica gel column chromatography, using 40:1and 20:1 by volume mixtures of ethyl acetate and ethanol as the eluent.The solvent was removed from the eluate by evaporation under reducedpressure, and the residue was recrystallized from methanol to obtain0.63 g of the title compound as yellow crystals, melting at 87 to 89° C.

EXAMPLE 104 6-(1,2-Dithiolan-3-yl)hexanoic acid (Compound No. 1-1467)##STR118##

30 ml of water and 60 ml of aqueous hydrochloric acid were added to 7.16g of 6-(2-oxo-1,3-dithian-4-yl)hexanenitrile, and the mixture was heatedunder reflux for 5 hours. The reaction mixture was then left to stand atroom temperature overnight, after which it was heated under reflux for 2hours and 30 minutes. The solvent was then removed from the reactionmixture by evaporation under reduced pressure, and water was added tothe residue, which was then extracted with ethyl acetate. The extractionsolution was washed with a saturated aqueous solution of sodium chlorideand dried over anhydrous sodium sulfate. The ethyl acetate was removedfrom the extraction solution by evaporation under reduced pressure, and150 ml of 1N aqueous solution of sodium hydroxide, 40 ml of 2N aqueoushydrochloric acid and 10 drops of a 1% w/v aqueous solution of ferricchloride were added to the residue. The mixture was then stirred at roomtemperature for 2 hours and 30 minutes while air was blown through it.The solvent was removed from the reaction mixture by evaporation underreduced pressure, and water was added to the residue, after which it waswashed with ethyl acetate. The aqueous layer was neutralized by theaddition of 2N aqueous hydrochloric acid, and ethyl acetate was added tothe solution. The aqueous layer (a) and ethyl acetate layer were thenseparated from the mixture.

The ethyl acetate layer was washed with a saturated aqueous solution ofsodium chloride and dried over anhydrous sodium sulfate. The ethylacetate was removed from the extraction solution by evaporation underreduced pressure, and the residue was subjected to silica gel columnchromatography, using a 1:1 by volume mixture of ethyl acetate andhexane as the eluent. The solvent was removed from the eluate byevaporation under reduced pressure, and the residue was dissolved in 40ml of toluene.

The ethyl acetate was evaporated from the ethyl acetate layer liberatedfrom the above aqueous layer (a), and 90 ml of a 1 N aqueous solution ofsodium hydroxide, 17 ml of 2 N aqueous hydrochloric acid and 5 drops ofa 1% w/v aqueous solution of ferric chloride were added to the residue,and then the mixture was stirred at room temperature for 1 hour whileair was blown through the mixture. The reaction mixture was left tostand at room temperature overnight, and the solvent was removed fromthe reaction mixture by evaporation under reduced pressure. Water wasadded to the residue, and the mixture was washed with ethyl acetate. Theaqueous layer was neutralized by the addition of 2 N aqueoushydrochloric acid and extracted with ethyl acetate. The extractionsolution was washed with a saturated aqueous solution of sodium chlorideand dried over anhydrous sodium sulfate. The extraction solution wascombined with the above-mentioned toluene solution, and the solvent wasremoved from the solution by evaporation under reduced pressure. Theresidue was subjected to reverse phase preparation silica gel columnchromatography, using 2:3, 1:1 and 3:2 by volume mixtures ofacetonitrile and water as eluent, and acetonitrile was removed from thesolution by evaporation under reduced pressure, after which the residuewas extracted with ethyl acetate. The extraction solution was washedwith a saturated aqueous solution of sodium chloride and dried overanhydrous sodium sulfate. The ethyl acetate was removed from theextraction solution by evaporation under reduced pressure, and theresidue was dissolved in 50 ml of toluene. The toluene was evaporatedfrom 2 ml of the resulting toluene solution, and the residue wasdissolved in dioxane and then lyophilised, to obtain 69 mg of the titlecompound as a yellow oil having an Rf value of 0.39 (silica gel thinlayer chromatography; using a 1:1 by volume mixture of ethyl acetate andhexane as developing solvent).

EXAMPLE 105 Methyl 6-(1,2-dithiolan-3-yl)hexanoylaminoacetate (CompoundNo. 1-1347) ##STR119##

The reaction was carried out as described in Example 47, but using 5 mlof a solution of 1.6 mmol of 6-(1,2-dithiolan-3-yl)hexanoic acid(prepared as described in Example 104) in toluene, 7 ml of anhydrousdimethylformamide, 373 mg of N,N'-carbonyldiimidazole, 0.25 ml oftriethylamine and 199 mg of glycine methyl ester hydrochloride. Thesolvent was removed from the reaction mixture by evaporation underreduced pressure, and water was added to the residue, after which it wasextracted with ethyl acetate. The extraction solution was washed with asaturated aqueous solution of sodium chloride and dried over anhydroussodium sulfate. The ethyl acetate was removed from the extractionsolution by evaporation under reduced pressure, and the residue wassubjected to silica gel column chromatography, using 2:1 and 3:1 byvolume mixtures of ethyl acetate and hexane as the eluent. The residuewas then subjected to reverse phase preparative silica gel columnchromatography, using 2:3 and 1:1 by volume mixtures of acetonitrile andwater as eluent, and the acetonitrile was removed from the solution byevaporation under reduced pressure, after which the residue wasextracted with ethyl acetate. The extraction solution was washed with asaturated aqueous solution of sodium chloride and dried over anhydroussodium sulfate. The ethyl acetate was removed from the extractionsolution by evaporation under reduced pressure, and the residue wasdissolved in dioxane and then lyophilised, to obtain 61 mg of the titlecompound as a pale yellow amorphous substance having an Rf value of 0.28(silica gel thin layer chromatography; using 2:1 by volume mixture ofethyl acetate and hexane as developing solvent).

EXAMPLE 106 Methyl2(S)-{N-[5-(1,2-dithiolan-3-yl)pentanoly]-N-methylamino}propionate(Compound No. 1-1224) ##STR120##

The reaction was carried out as described in Example 47, but using 500mg of D,L-α-lipoic acid, 13 ml of anhydrous dimethylformamide, 422 mg ofN,N'-carbonyldiimidazole, 0.36 ml of triethylamine and 399 mg ofN-methyl-L-alanine methyl ester hydrochloride. The solvent was removedfrom the reaction mixture by evaporation under reduced pressure, andwater was added to the residue, after which it was extracted with ethylacetate. The extraction solution was washed with a saturated aqueoussolution of sodium chloride and dried out anhydrous sodium sulfate. Theethyl acetate was removed from the extraction solution by evaporationunder reduced pressure, and the residue was subjected to silica gelcolumn chromatography, using 3:1 and 1:0 by volume mixtures of ethylacetate and hexane as the eluent. The solvent was evaporated from theeluate, and the residue was dissolved in dioxane and then lyophilised,to obtain 374 mg of the title compound as a yellow oil having an Rfvalue of 0.29 (silica gel thin layer chromatography; using ethyl acetateas developing solvent).

EXAMPLE 107 N-[6-(1,2-Dithiolan-3-yl)hexanoly]methanesulfonamide(Compound No. 1-1796) ##STR121##

6 ml of anhydrous dimethylformamide and 276 mg ofN,N'-carbonyldiimidazole were added to 10 ml of a solution of 1.5 mmolof 6-(1,2-dithiolan-3-yl)hexanoic acid (prepared as described in Example104) in toluene, and the mixture was stirred at room temperature for 4hours and 30 minutes. 162 mg of methanesulfanamide and 74 mg of sodiumhydride (as a 55% w/w dispersion in mineral oil) were then added to thereaction solution, and the mixture was stirred at room temperature for 1hour. The reaction mixture was then left to stand at room temperatureovernight, and the solvent was removed from the reaction mixture byevaporation under reduced pressure. Water was added to the residue, andthe mixture was washed with ethyl acetate and neutralized by theaddition of 2 N aqueous hydrochloric acid, after which it was extractedwith ethyl acetate. The extraction solution was washed with a saturatedaqueous solution of sodium chloride and dried over anhydrous sodiumsulfate. The ethyl acetate was removed from the extraction solution byevaporation under reduced pressure, and the residue was subjected tosilica gel column chromatography, using a 2:1 by volume mixture of ethylacetate and hexane as the eluent). The solvent was evaporated from theeluate, and the residue was again subjected to silica gel columnchromatography, using 2:3 and 3:2 by volume mixtures of ethyl acetateand hexane as the eluent. The solvent was removed from the eluate byevaporation under reduced pressure, and the residue was dissolved indioxane and then lyophilised, to obtain 98 mg of the title compound as ayellow oil having an Rf value of 0.37 (silica gel thin layerchromatography; using a 3:2 by volume mixture of ethyl acetate andhexane as developing solvent).

EXAMPLE 108 Methyl 3-[5-(1,2-dithiolan-3-yl)pentyl]ureidoacetate(Compound No. 1-2039) ##STR122##

The reaction was carried out as described in Example 46, but using 10 mlof a solution of 1.5 mmol of 6-(1,2-dithiolan-3-yl)hexanoic acid(prepared as described in Example 104) in toluene, 6 ml of anhydroustoluene, 0.42 ml of triethylamine, 0.39 ml of diphenylphosphoryl azide,6 ml of anhydrous dimethylformamide and 254 mg of glycine methyl esterhydrochloride. The solvent was removed from the reaction mixture byevaporation under reduced pressure, and water was added to the residue,after which it was extracted with ethyl acetate. The extraction solutionwas washed with a saturated aqueous solution of sodium chloride anddried over anhydrous sodium sulfate. The ethyl acetate was removed fromthe extraction solution by evaporation under reduced pressure, and theresidue was subjected to silica gel column chromatography, using 1:4 and3:2 by volume mixtures of ethyl acetate and hexane as the eluent. Thesolvent was removed from the eluate by evaporation under reducedpressure, and the residue was dissolved in dioxane and then lyophilised,to obtain 16 mg of the title compound as yellow crystals having an Rfvalue of 0.62 (silica gel thin layer chromatography; using a 2:3 byvolume mixture of ethyl acetate and hexane as developing solvent).

EXAMPLE 109 Ethyl 3-[4-(1,2-dithiolan-3-yl)butyl]-1-methylureidoacetate(Compound No. 1-820 Ethyl Ester) ##STR123##

The reaction was carried out as described in Example 46, but using 500mg of D,L-α-lipoic acid, 10 ml of anhydrous toluene, 0.73 ml oftriethylamine, 0.56 ml of diphenylphosphoryl azide, 10 ml of anhydroustetrahydrofuran and 399 mg of sarcosine ethyl ester hydrochloride. Thesolvent was removed from the reaction mixture by evaporation underreduced pressure, and water was added to the residue, after which it wasextracted with ethyl acetate. The extraction solution was washed with asaturated aqueous solution of sodium chloride and dried over anhydroussodium sulfate. The ethyl acetate was removed from the extractionsolution by evaporation under reduced pressure, and the residue wassubjected to silica gel column chromatography, using 2:1 and 1:0 byvolume mixtures of ethyl acetate and hexane as the eluent. The residuewas then subjected to reverse phase preparative silica gel columnchromatography, using 7:13, 2:3 and 1:1 by volume mixtures ofacetonitrile and water as eluent, and acetonitrile was removed from thesolution by evaporation under reduced pressure, after which the residuewas extracted with ethyl acetate. The extraction solution was washedwith a saturated aqueous solution of sodium chloride and dried overanhydrous sodium sulfate. The ethyl acetate was removed from theextraction solution by evaporation under reduced pressure, and theresidue was dissolved in dioxane and then lyophilised, to obtain 194 mgof the title compound as a pale yellow amorphous substance having an Rfvalue of 0.43 (silica gel thin layer chromatography, using ethyl acetateas developing solvent).

EXAMPLE 1103-[4-(1,2-Dithiolan-3-yl)butyl]-1,5(S)-dimethylimidazolidine-2,4-dione(Compound No. 1-2682) ##STR124##

The reaction was carried out as described in Example 46, but using 500mg of D,L-α-lipoic acid, 10 ml of anhydrous toluene, 0.73 ml oftriethylamine, 0.56 ml of diphenylphosphoryl azide, 5 ml of anhydroustetrahydrofuran, 5 ml of anhydrous dimethylformamide and 399 mg ofN-methyl-L-alanine methyl ester hydrochloride. The solvent was removedfrom the reaction mixture by evaporation under reduced pressure, andwater was added to the residue, after which it was extracted with ethylacetate. The extraction solution was washed with a saturated aqueoussolution of sodium chloride and dried over anhydrous sodium sulfate. Theethyl acetate was removed from the extraction solution by evaporationunder reduced pressure, and the residue was subjected to silica gelcolumn chromatography, using 3:2 and 1:1 by volume mixtures of ethylacetate and hexane as the eluent. The residue was then subjected toreverse phase preparative silica gel column chromatography, using 2:3and 1:1 by volume mixtures of acetonitrile and water as eluent, and theacetonitrile was removed from the solution by evaporation under reducedpressure, after which the residue was extracted with ethyl acetate. Theextraction solution was washed with a saturated aqueous solution ofsodium chloride and dried over anhydrous sodium sulfate. The ethylacetate was removed from the extraction solution by evaporation underreduced pressure, and the residue was dissolved in dioxane and thenlyophilised, to obtain 283 mg of the title compound as a yellow oilhaving an Rf value 0.29 (silica gel thin layer chromatography, using a3:2 by volume mixture of ethyl acetate and hexane as developingsolvent).

EXAMPLE 111 Methyl4-{3-[4-(1,2-dithiolan-3-yl)butyl]-1-methylureido}butanoate (CompoundNo. 1-2670 Methyl Ester) ##STR125##

The reaction was carried out as described in Example 46, but using 500mg of D,L-α-lipoic acid, 10 ml of anhydrous toluene, 0.73 ml oftriethylamine, 0.56 ml of diphenylphosphoryl azide, 5 ml of anhydrousdimethylformamide and 477 mg of methyl 4-(methylamino)butanoatehydrochloride. The solvent was removed from the reaction mixture byevaporation under reduced pressure, and water was added to the residue,after which it was extracted with ethyl acetate. The extraction solutionwas washed with a saturated aqueous solution of sodium chloride anddried over anhydrous sodium sulfate. The ethyl acetate was removed fromthe extraction solution by evaporation under reduced pressure, and theresidue was subjected to silica gel column chromatography, using 1:0 and20:1 by volume mixtures of ethyl acetate and methanol as the eluent. Thesolvent was removed from the eluate by evaporation under reducedpressure, and the residue was dissolved in dioxane and then lyophilised,to obtain 589 mg of the title compound as a pale yellow amorphoussubstance having an Rf value of 0.47 (silica gel thin layerchromatography, using a 20:1 by volume mixture of ethyl acetate andmethanol as the developing solvent).

EXAMPLE 112 N-[6-(1,2-Dithiolan-3-yl)hexanoyl]sulfamide (Compound No.1-1839) ##STR126##

The reaction was carried out as described in Example 107, but using 5 mlof a solution of 1.6 mmol of 6(1,2-dithiolan-3-yl)hexanoic acid(prepared as described in Example 104) in toluene, 7 ml of anhydrousdimethylformamide, 308 mg of N,N'-carbonyldiimidazole, 365 mg ofsulfamide and 83 mg of sodium hydride (as a 55% w/w dispersion inmineral oil). The solvent was removed from the reaction mixture byevaporation under reduced pressure, and water was added to the residue,after which it was extracted with ethyl acetate. The extraction solutionwas washed with a saturated aqueous solution of sodium chloride anddried over anhydrous sodium sulfate. The ethyl acetate was removed fromthe extraction solution by evaporation under reduced pressure, and theresidue was subjected to silica gel column chromatography, using 3:2 and2:1 by volume mixtures of ethyl acetate and hexane as the eluent. Thesolvent was removed from the eluate by evaporation under reducedpressure, and the residue was recrystallized from a 1:2 by volumemixture of ethyl acetate and hexane, to obtain 92 mg of the titlecompound as pale yellow crystals, melting at 130 to 132° C.

EXAMPLE 113N-{3-[4-(1,2-Dithiolan-3-yl)butyl]ureidoacetyl}methanesulfonamide(Compound No. 1-2643) ##STR127##

The reaction was carried out as described in Example 73, but using 201mg of methyl 3-[4-(1,2-dithiolan-3-yl)butyl]ureidoacetate (prepared asdescribed in Example 46), 4 ml of anhydrous dimethylformamide, 129 mg ofN,N'-carbonyldiimidazole. 76 mg of methanesulfanomide and 35 mg ofsodium hydride (as a 55% w/w dispersion in mineral oil). The solvent wasremoved from the reaction mixture by evaporation under reduced pressure,and water was added to the residue. The mixture was neutralized by theaddition of 2 N aqueous hydrochloric acid, after which it was extractedwith ethyl acetate. The extraction solution was washed with a saturatedaqueous solution of sodium chloride and dried over anhydrous sodiumsulfate. The ethyl acetate was removed from the extraction solution byevaporation under reduced pressure, and the residue was recrystallizedfrom methanol, to obtain 150 mg of the title compound as white crystals,melting at 157 to 158° C.

EXAMPLE 114 N-{3-[4-(1,2-Dithiolan-3-yl)butyl]ureidoacetyl}sulfamide(Compound No. 1-2647) ##STR128##

The reaction was carried out as described in Example 73, but using 0.20g of 3-[4-(1,2-dithiolan-3-yl)butyl]ureidoacetic acid (prepared asdescribed in Example 48), 4 ml of anhydrous dimethylformamide, 0.13 g ofN,N'-carbonyldiimidazole, 0.15 g of sulfamide and 0.04 g of sodiumhydride (as a 55% w/w dispersion in mineral oil). The solvent wasremoved from the reaction mixture by evaporation under reduced pressure,and water was added to the residue. The mixture was neutralized by theaddition of 2 N aqueous hydrochloric acid, after which it was extractedwith ethyl acetate. The extraction solution was washed with a saturatedaqueous solution of sodium chloride and dried over anhydrous sodiumsulfate. The ethyl acetate was removed from the extraction solution byevaporation under reduced pressure, and the residue was recrystallizedfrom a mixture of methanol and ethyl acetate, to obtain 76 mg of thetitle compound as yellow crystals, melting at 143 to 145° C.

EXAMPLE 115N-(2(R)-{3-[4-(1,2-Dithiolan-3-yl)butyl]ureido}propionyl)sulfamide(Compound No. 1-2655) ##STR129##

The reaction was carried out as described in Example 73, but using 0.21g of 2(R)-{3-[4-(1,2-dithiolan-3-yl)butyl]ureido}propionic acid(prepared as described in Example 71), 5 ml of anhydrousdimethylformamide, 0.13 g of N,N'-carbonyldiimidazole, 0.15 g ofsulfamide and 0.04 g of sodium hydride (as a 55% w/w dispersion inmineral oil). The solvent was removed from the reaction mixture byevaporation under reduced pressure, and water was added to the residue.The mixture was neutralized by the addition of 2 N aqueous hydrochloricacid, after which it was extracted with ethyl acetate. The extractionsolution was washed with a saturated aqueous solution of sodium chlorideand dried over anhydrous sodium sulfate. The ethyl acetate was removedfrom the extraction solution by evaporation under reduced pressure, andthe residue was recrystallized from ethyl acetate, to obtain 114 mg ofthe title compound as a pale yellow powder, melting at 156 to 157° C.

EXAMPLE 116N-(2(S)-{3-[4-(1,2-Dithiolan-3-yl)butyl]ureido}propionyl)methanesulfanamide(Compound No. 1-2655) ##STR130##

The reaction was carried out as described in Example 73, but using 0.13g of 2(S)-{3-[4-(1,2-dithiolan-3-yl)butyl]ureido}propionic acid(prepared as described in Example 52), 4 ml of anhydrousdimethylformamide, 0.08 g of N,N'-carbonyldiimidazole, 0.05 g ofmethanesulfanomide and 0.02 g of sodium hydride (as a 55% w/w dispersionin mineral oil). The solvent was removed from the reaction mixture byevaporation under reduced pressure, and water was added to the residue.The mixture was neutralized by the addition of 2 N aqueous hydrochloricacid, after which it was extracted with ethyl acetate. The extractionsolution was washed with a saturated aqueous solution of sodium chlorideand dried over anhydrous sodium sulfate. The ethyl acetate was removedfrom the extraction solution by evaporation under reduced pressure, andthe residue was recrystallized from ethyl acetate, to obtain 80 mg ofthe title compound as a white powder, melting at 142 to 147° C.

EXAMPLE 117 4-{3-[4-(1,2-Dithiolan-3-yl)butyl]ureido}butanoic Acid(Compound No. 1-1276) ##STR131##

The reaction was carried out as described in Example 48, but using 0.65g of methyl 4-{3-[4-(1,2-dithiolan-3-yl)butyl]ureido}butanoate (preparedas described in Example 75), 13 ml of methanol and 7.10 ml of a 1 Naqueous solution of sodium hydroxide. The solvent was removed from thereaction mixture by evaporation under reduced pressure, and water wasadded to the residue. The mixture was neutralized by the addition of 2 Naqueous hydrochloric acid, after which it was extracted with ethylacetate. The extraction solution was washed with a saturated aqueoussolution of sodium chloride and dried over anhydrous sodium sulfate. Theethyl acetate was removed from the extraction solution by evaporationunder reduced pressure, and the residue was recrystallized from ethylacetate, to obtain 0.46 g of the title compound as a pale yellow powder,melting at 94 to 99° C.

EXAMPLE 118 Methyl-5-[5-(1,2-dithiolan-3-yl)pentanoylamino]pentanoate(Compound No. 1-2657 Methyl Ester) ##STR132##

The reaction was carried out as described in Example 47, but using 1.00g of D,L-α-lipoic acid, 40 ml of anhydrous dimethylformamide, 0.86 g ofN,N'-carbonyldiimidazole, 0.74 ml of triethylamine and 0.89 g of methyl5-aminopentanoate hydrochloride. The solvent was removed form thereaction mixture by evaporation under reduced pressure, and water wasadded to the residue, after which it was extracted with ethyl acetate.The extraction solution was washed with a saturated aqueous solution ofsodium chloride and dried over anhydrous sodium sulfate. The ethylacetate was removed from the extraction solution by evaporation underreduced pressure, and the residue was subjected to silica gel columnchromatography, using 2:1 and 1:0 by volume mixtures of ethyl acetateand hexane as the eluent. It was then recrystallized from ethyl acetate,to obtain 1.10 g of the title compound as pale yellow crystals, meltingat 60 to 62° C.

EXAMPLE 119 Methyl 5-{3-[4-(1,2-dithiolan-3-yl)butyl]ureido}pentanoate(Compound No. 1-2659 Methyl Ester) ##STR133##

The reaction was carried out as described in Example 46, but using 1.00g of D,L-α-lipoic acid, 20 ml of anhydrous toluene, 1.48 ml oftriethylamine, 1.15 ml of diphenylphosphoryl azide and 0.81 g of methyl5-aminopentanoate hydrochloride. The solvent was removed from thereaction mixture by evaporation under reduced pressure, and water wasadded to the residue, after which it was extracted with ethyl acetate.The extraction solution was washed with a saturated aqueous solution ofsodium chloride and dried over anhydrous sodium sulfate. The ethylacetate was removed from the extraction solution by evaporation underreduced pressure, and the residue was subjected to silica gel columnchromatography, using a 2:1 by volume mixture of ethyl acetate andhexane, followed by a 9:1 by volume mixture of ethyl acetate andethanol, as the eluent, to obtain 1.27 g of the title compound as a paleyellow powder, melting at 90 to 92° C.

EXAMPLE 120 5-[5-(1,2-Dithiolan-3-yl)pentanoylamino]pentanoic Acid(Compound No. 1-2657) ##STR134##

The reaction was carried out as described in Example 49, but using 0.65g of methyl 5-[5-(1,2-dithiolan-3-yl)pentanoylamino]pentanoate (preparedas described in Example 118), 13 ml of methanol and 5.09 ml of a 1 Naqueous solution of sodium hydroxide. The solvent was removed from thereaction mixture by evaporation under reduced pressure, and water wasadded to the residue. The mixture was neutralized by the addition of 2 Naqueous hydrochloric acid, after which it was extracted with ethylacetate. The extraction solution was washed with a saturated aqueoussolution of sodium chloride and dried over anhydrous sodium sulfate. Theethyl acetate was removed from the extraction solution by evaporationunder reduced pressure, and the residue was recrystallized from ethylacetate, to obtain 0.33 g of the title compound as pale yellowish greencrystals, melting at 98 to 100° C.

EXAMPLE 121 5-{3-[4-(1,2-Dithiolan-3-yl)butyl]ureido}pentanoic Acid(Compound No. 1-2659) ##STR135##

The reaction was carried out as described in Example 48, but using 0.30g of methyl 5-{3-[4-(1,2-dithiolan-3-yl)butyl]ureido}pentanoate(prepared as described in Example 119), 10 ml of methanol and 3.14 ml ofa 1 N aqueous solution of sodium hydroxide. The solvent was removed fromthe reaction mixture by evaporation under reduced pressure, and waterwas added to the residue. The mixture was neutralized by the addition of2 N aqueous hydrochloric acid, after which it was extracted with ethylacetate. The extraction solution was washed with a saturated aqueoussolution of sodium chloride and dried over anhydrous sodium sulfate. Theethyl acetate was removed from the extraction solution by evaporationunder reduced pressure, and the residue was recrystallized from ethylacetate, to obtain 0.23 g of the title compound as pale yellow crystals,melting at 125 to 132° C.

EXAMPLE 122 5-(1,2-Dithiolan-3yl)-N-(2-hydroxyethyl)pentanamide(Compound No. 1-2661) ##STR136##

0.86 g of N,N'-carbonyldiimidazole was added to 20 ml of a solution of1.00 g of D,L-α-lipoic acid in anhydrous dimethylformamide, and themixture was stirred at room temperature for 1 hour and 20 minutes. 0.32ml of 2-aminoethanol was then added to the reaction solution, and theresulting mixture was stirred at room temperature for 4 hours and 10minutes. The solvent was then removed from the reaction mixture byevaporation under reduced pressure, and water was added to the residue,after which it was extracted with ethyl acetate. The extraction solutionwas washed with a saturated aqueous solution of sodium chloride anddried over anhydrous sodium sulfate. The ethyl acetate was removed fromthe extraction solution by evaporation under reduced pressure, and theresidue was subjected to silica gel column chromatography, using a 19:1by volume mixture of ethyl acetate and ethanol as the eluent. Thesolvent was removed from the eluate by evaporation under reducedpressure, and the residue was dissolved in dioxane and then lyophilised,to obtain 0.71 g of the title compound as a yellow amorphous substancehaving an Rf value of 0.38 (silica gel thin layer chromatography, usinga 19:1 by volume mixture of ethyl acetate and ethanol as developingsolvent).

EXAMPLE 1235-(1,2-Dithiolan-3-yl)-N-(2-hydroxy-1-methylethyl)pentanamide (CompoundNo. 1-2665) ##STR137##

The reaction was carried out as described in Example 122, but using 1.00g of D,L-α-lipoic acid, 20 ml of anhydrous dimethylformamide, 0.86 g ofN,N'-carbonyldiimidazole and 0.42 ml of D,L-alaninol. The solvent wasremoved from the reaction mixture by evaporation under reduced pressure,and water was added to the residue, after which it was extracted withethyl acetate. The extraction solution was washed with a saturatedaqueous solution of sodium chloride and dried over anhydrous sodiumsulfate. The ethyl acetate was removed from the extraction solution byevaporation under reduced pressure, and the residue was subjected tosilica gel column chromatography, using ethyl acetate as the eluent. Thesolvent was removed from the eluate by evaporation under reducedpressure, and the residue was dissolved in dioxane and lyophilised, toobtain 0.39 g of the title compound as a yellow amorphous substance,melting at 52 to 56° C.

EXAMPLE 124 N-[4-(1,2-Dithiolan-3-yl)butyl]-N'-(2-hydroxyethyl)urea(Compound No. 1-2663) ##STR138##

The reaction was carried out as described in Example 46, but using 1.00g of D,L-α-lipoic acid, 20 ml of anhydrous toluene, 0.74 ml oftriethylamine, 1.15 ml of diphenylphosphoryl azide and 0.29 ml of2-hydroxy-1-ethylamine. The solvent was removed from the reactionmixture by evaporation under reduced pressure, and water was added tothe residue, after which it was extracted with ethyl acetate. Theextraction solution was washed with a saturated aqueous solution ofsodium chloride and dried over anhydrous sodium sulfate. The ethylacetate was removed from the extraction solution by evaporation underreduced pressure, and the residue was subjected to silica gel columnchromatography, using 39:1 and 19:1 by volume mixtures of ethyl acetateand ethanol as the eluent. The solvent was removed from the eluate byevaporation under reduced pressure, and the residue was recrystallizedfrom methanol to obtain 352 mg of the title compound as yellow crystals,melting at 50 to 65° C.

EXAMPLE 125N-[5-(1,2-Dithiolan-3-yl)pentanoyl]-N-methylmethanesulfonamide (CompoundNo. 1-2672) ##STR139##

40 mg of copper chloride were added to 20 ml of a solution of 1.36 g ofdicyclohexylcarbodiimide in anhydrous methanol, and the mixture was leftto stand at room temperature for one and one half hours. The solvent wasthen removed from the mixture by distillation under reduced pressure. 20ml of anhydrous dimethylformamide and 1.00 g ofN-[5-(1,2-dithiolan-3-yl)pentanoyl]methanesulfonamide (prepared asdescribed in Example 2) were then added to the residue, and the mixturewas stirred at 70° C. on an oil bath for an hour. The mixture was thenleft to stand at room temperature overnight, after which it was stirredat 70° C. on an oil bath for 1 hour, and the solvent was removed fromthe reaction mixture by evaporation under reduced pressure. Water wasadded to the residue, and the mixture was extracted with ethyl acetate.Insoluble material in the extract was removed by filtration, and thefiltrate was washed with a saturated aqueous solution of sodium chlorideand dried over anhydrous sodium sulfate. The ethyl acetate was removedfrom the solution by evaporation under reduced pressure, and the residuewas subjected to silica gel column chromatography, using 2:3 and 1:1 byvolume mixtures of ethyl acetate and hexane as the eluent. The solventwas removed from the eluate by evaporation under reduced pressure, andthe residue was subjected to reverse phase preparative silica gel columnchromatography, using 1:1 and 3:2 by volume mixtures of acetonitrile andwater as eluent. The acetonitrile was then removed from the solution byevaporation under reduced pressure, after the residue was extracted withethyl acetate. The extracted solution was washed with a saturatedaqueous solution of sodium chloride and dried over anhydrous sodiumsulfate. The ethyl acetate was removed from the extraction solution byevaporation under reduced pressure, and the residue was dissolved indioxane and then lyophilised, to obtain 660 mg of the title compound asa pale yellow amorphous substance having an Rf value of 0.27 (silica gelthin layer chromatography, using a 2:3 by volume mixture of ethylacetate and hexane as developing solvent).

EXAMPLE 126 Allyl N-[4-(1,2-dithiolan-3-yl)butyl]carbamate ##STR140##

The reaction was carried out as described in Example 31, but using 1.00g of D,L-α-lipoic acid, 10 ml of anhydrous toluene, 0.73 ml oftriethylamine, 1.14 ml of diphenylphosphoryl azide and 2 ml of allylalcohol. The reaction mixture was washed with water, the water layer waswashed with ethyl acetate, and the ethyl acetate washings were combinedwith the above-mentioned toluene solution. The extract was washed with asaturated aqueous solution of sodium chloride and dried over anhydroussodium sulfate. The solvent was removed from the extract by evaporationunder reduced pressure, and the residue was subjected to silica gelcolumn chromatography, using 1:4 and 1:2 by volume mixtures of ethylacetate and hexane as the eluent. The solvent was removed from theeluate by evaporation under reduced pressure, and the residue wasdissolved in dioxane and then lyophilised, to obtain 944 mg of the titlecompound as an oily yellow substance having an Rf value of 0.49 (silicagel thin layer chromatography, using a 1:2 by volume mixture of ethylacetate and hexane as developing solvent).

PREPARATION 1 5(1,2-Dithiolan-3-yl)pentanol ##STR141##

44 ml of a hexane solution containing 2.0 M of(trimethylsilyl)diazomethane was added dropwise, whilst ice-cooling, toa mixture of 15.00 g of D,L-α-lipoic acid in 15 ml of methanol and 150ml of toluene, and then the mixture was stirred at room temperature forone hour. 11 ml of a hexane solution containing 2.0 M of(trimethylsilyl)diazomethane were then added dropwise to the reactionmixture. The resulting mixture was stirred at room temperature for 2hour. The reaction mixture was then allowed to stand at room temperaturefor 2 days. The solvent was then removed by distillation under reducedpressure from the reaction mixture, to give ethyl5-(1,2-dithiolan-3-yl)pentanoate as a yellow oil.

A solution of ethyl 5-(1,2-dithiolan-3-yl)pentanoate in 40 ml ofanhydrous tetrahydrofuran was added dropwise, whilst cooling with iceand sodium chloride, to a suspension of 3.34 g of lithium aluminumhydride in 150 ml of anhydrous tetrahydrofuran. The resulting mixturewas stirred at room temperature for 3 hours and 30 minutes. Sodiumsulfate decahydrate was then added, whilst cooling with ice and sodiumchloride, to the reaction mixture, and then the mixture was stirred atroom temperature for 3 hours. The reaction mixture was allowed to standovernight at room temperature, and then insoluble matter was filteredoff using a Celite (trade mark) filter aid. The solvent was removed fromthe filtrate by distillation under reduced pressure. 50 ml of methanol,25 ml of a 1 N aqueous solution of sodium hydroxide and 10 ml of 2 Naqueous hydrochloric acid were then added to the residue. Air was thenblown into the resulting mixture. Five drops of a 1% aqueous solution offerric chloride were added dropwise to the reaction mixture, and thenthe mixture was stirred at room temperature for one hour. The reactionmixture was allowed to stand overnight at room temperature, and then thesolvent was removed by distillation under reduced pressure. Water wasadded to the residue, after which it was extracted with ethyl acetate.The extract was washed with a saturated aqueous solution of sodiumchloride and then dried over anhydrous sodium sulfate. Ethyl acetate wasremoved from the extract by distillation under reduced pressure, and theresidue was subjected to silica gel column chromatography, using 1:2 and1:1 by volume mixtures of ethyl acetate and hexane as eluent. Thesolvent was removed from the resulting eluate by distillation underreduced pressure, and 30 ml of toluene were added to the residue. 1 mlwas taken from the resulting solution, and the solvent was removed bydistillation under reduced pressure, to give 0.13 g of the titlecompound as a yellow oil having an Rf value of 0.39 (silica gel thinlayer chromatography; using a 1:1 by volume mixture of ethyl acetate andhexane as the eluent).

We claim:
 1. A compound of formula (I): ##STR142## wherein one of m andn represents 0, and the other represents 0, 1 or 2;k represents 0 or aninteger of from 1 to 12; R¹ represents:a hydrogen atom; a substituent αselected from the group consisting of an unsubstituted aryl, anunsubstituted heterocyclic group, an aryl group substituted by 1 to 3substituents β and a heterocyclic group substituted with 1 to 3substituents β, wherein said substituents β are selected from the groupconsisting of an unsubstitued lower alkyl group, a halogenated loweralkyl group, a lower alkoxy group, a lower alkylthio group, a hydroxygroup, a carboxy group, a carbamoyl group of which the nitrogen atomthereof is unsubstituted or substituted, a lower alkoxycarbonyl group, ahalogen atom, a nitro group, an amine residue, a sulfo group, asulfamoyl group, a cyano group and a hydroxy-substituted lower alkylgroup; an alkyl group having from 1 to 12 carbon atoms which isunsubstituted or is substituted from 1 to 3 substituents selected fromthe group consisting of said substituent α and a substituent γ selectedfrom the group consisting of a lower alkoxy group, a lower alkylthiogroup, a hydroxy group, a nitrooxy group, a carboxy group, a loweralkoxycarbonyl group, a halogen atom, a sulfo group, a sulfamoyl group,an amine residue, and a carbamoyl group of which the nitrogen atomthereof is unsubstituted or substituted, or said unsubstituted orsubstituted alkyl group in which the carbon chain thereof is interruptedby an oxygen atom, a sulfur atom or both an oxygen atom and a sulfuratom; a group of the formula --OR⁷, wherein R⁷ represents a lower alkylgroup, a lower alkenyl group, an unsubstituted aralyl group, an arakylgroup of which the aryl moiety thereof is substituted with 1 to 3 groupsselected from the group consisting of said substituents β or a groupselected from the group consisting of said substituents α; or a hydroxygroup; A represents --CON(R²)SO₂₋₋, wherein R² represents a hydrogenatom, an alkyl group having from 1 to 12 carbon atoms, an unsubstitutedaralkyl group, an acyl group, an aralkyl group of which the aryl moietythereof is substituted with from 1 to 3 groups selected from the groupconsisting of said substituents β, or R² is a group selected from thegroup consisting of said substitutents α; and B represents a singlebond; or a pharmaceutically acceptable salt thereof.
 2. A compound ofclaim 1, represented by the formula (I'): ##STR143## or apharmaceutically acceptable salt thereof.
 3. A compound of claim 1,wherein one of m and n is 0, and the other is 0 or
 1. 4. A compound ofclaim 1, wherein k is 0 or an integer of from 1 to
 8. 5. A compound ofclaim 1, wherein R¹ represents a heterocyclic group, an alkyl grouphaving from 1 to 12 carbon atoms which is unsubstituted or issubstituted by from 1 to 3 substitutents selected from the groupconsisting of said substituents α and said substituents γ or R¹ is saidunsubstituted or unsubstituted alkyl group in which the carbon chainthereof is interrupted by an oxygen atom, a sulfur atom or both anoxygen atom and a sulfur atom.
 6. A compound of claim 1, wherein R¹represents a hydroxy group or an alkoxy group having from 1 to 5 carbonatoms.
 7. A compound of claim 1, wherein R² represents a hydrogen atom,an alkyl group having from 1 to 12 carbon atoms or a benzyl group.
 8. Acompound of claim 2, wherein one of m and n is 0, and the other is 0or
 1. 9. A compound of claim 2, wherein k is 0 or an integer of from 1to
 8. 10. A compound of claim 2, wherein R¹ represents a heterocyclicgroup, an alkyl group having from 1 to 12 carbon atoms which isunsubstituted or is substituted by from 1 to 3 substituents selectedfrom the group consisting of said substitutents α and said substitutentsγ or R¹ is said unsubstituted or substituted alkyl group in which thecarbon chain thereof is interrupted by an oxygen atom, a sulfur atom orboth an oxygen atom and a sulfur atom.
 11. A compound of claim 2,wherein R¹ represents a hydroxy group or an alkoxy group having from 1to 5 carbon atoms.
 12. A compound of claim 2, wherein R² represents ahydrogen atom, an alkyl group having from 1 to 12 carbon atoms or abenzyl group.
 13. A compound of claim 1, wherein:one or m and n is 0,and the other is 0 is 1; k is 0 or an integer of from 1 to 8; R¹represents a heterocyclic group, a hydroxy group, an alkoxy group havingfrom 1 to 5 carbon atoms, an alkyl group having from 1 to 12 carbonatoms which is unsubstituted or is substituted by from 1 to 3substituents selected from the group consisting of said substituents αand said substituents γ or R¹ is said unsubstituted or substituted alkylgroup in which the carbon chain thereof is interrupted by an oxygenatom, a sulfur atom or both an oxygen atom and a sulfur atom, or R¹ is agroup of the formula --OR⁷ wherein R⁷ is a hydrogen atom or an alkylgroup having 1 to 5 carbon atoms; and R² represents a hydrogen atom, analkyl group having from 1 to 12 carbon atoms or a benzyl group.
 14. Acompound of claim 13, wherein said compound of formula (I) has theformula (I'): ##STR144##
 15. A compound of claim 1, wherein both of mand n are
 0. 16. A compound of claim 1, wherein k is an integer of from2 to
 6. 17. A compound of claim 1, wherein R¹ represents an alkyl grouphaving from 1 to 5 carbon atoms, an alkoxycarbonylalkyl group havingfrom 3 to 8 carbon atoms, a carboxyalkyl group having from 2 to 7 carbonatoms, a hydroxyalkyl group having from 2 to 5 carbon atoms, aheterocyclic group, an alkoxy group having from 1 to 5 carbon atoms or ahydroxy group.
 18. A compound of claim 1, wherein R² represents ahydrogen atom or an alkyl group having from 1 to 12 carbon atoms.
 19. Acompound of claim 2, wherein both of m and n are
 0. 20. A compound ofclaim 2, wherein k is an integer of from 2 to
 6. 21. A compound of claim2, wherein R¹ represents an alkyl group having from 1 to 5 carbon atoms,an alkoxycarbonylalkyl group having from 3 to 8 carbon atoms, acarboxyalkyl group having from 2 to 7 carbon atoms, a hydroxyalkyl grouphaving from 2 to 5 carbon atoms, a heterocyclic group, an alkoxy grouphaving from 1 to 5 carbon atoms or a hydroxy group.
 22. A compound ofclaim 2, wherein R² represents a hydrogen atom or an alkyl group havingfrom 1 to 12 carbon atoms.
 23. A compound of claim 1, wherein: both of mand n are 0;k is an integer of from 2 to 6; and R¹ represents an alkylgroup having from 1 to 5 carbon atoms, an alkoxycarbonylalkyl grouphaving from 3 to 8 carbon atoms, a carboxyalkyl group having from 2 to 7carbon atoms, a hydroxyalkyl group having from 2 to 5 carbon atoms, aheterocyclic group, an alkoxy group having from 1 to 5 carbon atoms or ahydroxy group R² represents a hydrogen atom or an alkyl group havingfrom 1 to 12 carbon atoms.
 24. A compound of claim 23, wherein saidcompound of formula (I) has the formula (I'): ##STR145##
 25. A compoundof claim 1, wherein k is 4 or
 5. 26. A compound of claim 1, wherein R¹represents an alkyl group having from 1 to 5 carbon atoms, analkoxycarbonylalkyl group having from 3 to 8 carbon atoms, acarboxyalkyl group having from 2 to 7 carbon atoms, a hydroxyalkyl grouphaving from 2 to 5 carbon atoms, a heterocyclic group or an alkoxy grouphaving from 1 to 5 carbon atoms.
 27. A compound of claim 1, wherein k is4 or
 5. 28. A compound of claim 2, wherein R¹ represents an alkyl grouphaving from 1 to 5 carbon atoms, an alkoxycarbonylalkyl group havingfrom 3 to 8 carbon atoms, a carboxyalkyl group having from 2 to 7 carbonatoms, a hydroxyalkyl group having from 2 to 5 carbon atoms, aheterocyclic group or an alkoxy group having from 1 to 5 carbon atoms.29. A compound of claim 1, wherein: both of m and n are 0;k is 4 or 5;and R¹ represents an alkyl group having from 1 to 5 carbon atoms, analkoxycarbonylalkyl group having from 3 to 8 carbon atoms, acarboxyalkyl group having from 2 to 7 carbon atoms, a hydroxyalkyl grouphaving from 2 to 5 carbon atoms, a heterocyclic group or an alkoxy grouphaving from 1 to 5 carbon atoms.
 30. A compound of claim 29, whereinsaid compound of formula (I) has the formula (I'): ##STR146##
 31. Acompound of claim 1, selected from the group consisting ofN-[5-(1,2-dithiolan-3-yl)pentanoyl]methanesulfonamide or apharmaceutically acceptable salt thereof.
 32. A method of enhancing theactivity of glutathione reductase in a mammal, comprising administeringto said mammal an effective amount of an active compound of the formula(I) according to claim 1, or a pharmaceutically acceptable salt thereof.33. A method of claim 32, wherein said active compound isN-[5-(1,2-dithiolan-3-yl)pentanoyl]methanesulfonamide or apharmaceutically acceptable salt thereof.
 34. A method for the treatmentor prevention of cataracts in a mammal comprising administering to saidmammal an effective amount of an active compound of the formula (I)according to claim 1, or a pharmaceutically acceptable salt thereof. 35.A method of claim 34, wherein said active compound isN-[5-(1,2-dithiolan-3-yl)pentanoyl]methanesulfonamide or apharmaceutically acceptable salt thereof.
 36. A method of claim 32,wherein: one of m and n is 0, and the other is 0 or 1;k is 0 or aninteger of from 1 to 8; R¹ represents a hydroxy group, an alkoxy grouphaving from 1 to 5 carbon atoms, a heterocyclic group, an alkyl grouphaving from 1 to 12 carbon atoms which is unsubstituted or issubstituted by from 1 to 3 substitutents selected from the groupconsisting of said substitutents α and said substitutents γ or R¹ issaid unsubstituted or substituted alkyl group in which the carbon chainthereof is interrupted by an oxygen atom, a sulfur atom or both anoxygen atom and a sulfur atom; and R² represents a hydrogen atom, analkyl group having from 1 to 12 carbon atoms or a benzyl group.
 37. Amethod of claim 36, wherein said compound of formula (I) has the formula(I'): ##STR147##
 38. A method of claim 32, wherein: both of m and n are0;k is an integer of from 2 to 6; and R¹ represents an alkyl grouphaving from 1 to 5 carbon atoms, an alkoxycarbonylalkyl group havingfrom 3 to 8 carbon atoms, a carboxyalkyl group having from 2 to 7 carbonatoms, a hydroxyalkyl group having from 2 to 5 carbon atoms, aheterocyclic group, an alkoxy group having from 1 to 5 carbon atoms or ahydroxy group; R² represents a hydrogen atom or an alkyl group havingfrom 1 to 12 carbon atoms.
 39. A method of claim 38, wherein saidcompound of formula (I) has the formula (I'): ##STR148##40.
 40. A methodof claim 32, wherein: both of m and n are 0;k is 4 or 5; and R¹represents an alkyl group having from 1 to 5 carbon atoms, analkoxycarbonylalkyl group having from 3 to 8 carbon atoms, acarboxyalkyl group having from 2 to 7 carbon atoms, a hydroxyalkyl grouphaving from 2 to 5 carbon atoms, a heterocyclic group or an alkoxy grouphaving from 1 to 5 carbon atoms.
 41. A method of claim 40, wherein saidcompound of formula (I) has the formula (I'): ##STR149##
 42. A method ofclaim 34, wherein: one or m and n is 0, and the other is 0 or 1;k is 0or an integer of from 1 to 8; and R¹ represents a hydroxy group, analkoxy group having from 1 to 5 carbon atoms, a heterocyclic group, analkyl group having from 1 to 12 carbon atoms which is unsubstituted oris substituted by from 1 to 3 substituents selected from the groupconsisting of said substituents α and said substituents γ or R¹ is saidunsubstituted or substituted alkyl group in which the carbon chainthereof is interrupted by an oxygen atom, a sulfur atom or both anoxygen atom and a sulfur atom.
 43. A method of claim 42, wherein saidcompound of formula (I) has the formula (I'): ##STR150##
 44. A method ofclaim 34, wherein: both of m and n are 0;k is an integer of from 2 to 6;and R¹ represents an alkyl group having from 1 to 5 carbon atoms, analkoxycarbonylalkyl group having from 3 to 8 carbon atoms, acarboxyalkyl group having from 2 to 7 carbon atoms, a hydroxyalkyl grouphaving from 2 to 5 carbon atoms, a heterocyclic group, an alkoxy grouphaving from 1 to 5 carbon atoms or a hydroxy group.
 45. A method ofclaim 44, wherein said compound of formula (I) has the formula (I'):##STR151##
 46. A method of claim 34, wherein: both m and n are 0;k is 4or 5; and R¹ represents an alkyl group having from 1 to 5 carbon atoms,an alkoxycarbonylalkyl group having from 3 to 8 carbon atoms, acarboxyalkyl group having from 2 to 7 carbon atoms, a hydroxyalkyl grouphaving from 2 to 5 carbon atoms, a heterocyclic group or an alkoxy grouphaving from 1 to 5 carbon atoms.
 47. A method of claim 46, wherein saidcompound of formula (I) has the formula (I'): ##STR152##